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CAS No. :	158021-47-7
Formula :	C₅₀H₉₉NO₉
M.W :	858.32
SMILES Code :	CCCCCCCCCCCCCCCCCCCCCCCCCC(N[C@@H](CO[C@@H]1[C@@H]([C@H]([C@H]([C@@H](CO)O1)O)O)O)[C@H](O)[C@H](O)CCCCCCCCCCCCCC)=O
Synonyms :	KRN7000; α-GalCer
MDL No. :	MFCD00939559

GHS Pictogram:
Signal Word:	Warning
Hazard Statements:	H315-H319
Precautionary Statements:	P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313

E. coli	25 µM	15 minutes	To determine the activity of αGalCer_GT, results showed that the enzyme forms αGalCer as a unique product and the reaction is complete after 15 min.	Int J Mol Sci. 2022 Nov 12;23(22):13975
RAW SR-A1 KO cells	1 µg/mL	18 hours	To test the role of SR-A1 in PLS-α-GalCer processing, results showed that the processing efficiency of PLS-α-GalCer was significantly reduced in SR-A1 KO cells.	J Immunother Cancer. 2025 Mar 22;13(3):e009539
RAW 264.7 cells (wild type)	1 µg/mL	18 hours	To test the efficiency of PLS-α-GalCer uptake and processing in APCs, results showed that PLS-α-GalCer was more efficiently internalized and processed by APCs than α-GalCer.	J Immunother Cancer. 2025 Mar 22;13(3):e009539
Mouse spleenic antigen presenting cells	1 ng/mL to 1 µg/mL	24 hours	To compare the presentation efficiency of nanoparticle and soluble forms of αGalCer in different antigen presenting cells. Results showed nanoparticle formulated αGalCer was presented 100-fold less efficiently by B cells compared to CD11c+ cells.	Vaccine. 2009 May 26;27(25-26):3484-8
HepG2 2.2.15 cells	1 to 100 nM	3 days	Inhibited HBV secretion with an IC50 of 0.4 ± 1.1 nM	Antimicrob Agents Chemother. 2004 Jun;48(6):2085-90
Spleen mononuclear cells	100 ng/mL	3 days	To evaluate the effect of α-GalCer on IL-2 production in spleen mononuclear cells. Results showed that α-GalCer promoted IL-2 production in WT mice but not in CD1d knockout mice.	J Cell Mol Med. 2019 Feb;23(2):1072-1085
Spleen mononuclear cells	100 ng/mL	3 days	To evaluate the effect of α-GalCer on IL-2 production, results showed that α-GalCer promoted IL-2 production in spleen mononuclear cells from WT mice but not in CD1d knockout mice.	J Cell Mol Med. 2019 Feb;23(2):1072-1085
Bone marrow-derived dendritic cells	5 μg/mL	3 days	To investigate the effect of α-GalCer on dendritic cell differentiation. The results showed that α-GalCer significantly increased the number of DEC-205+DCs while decreasing the number of 33D1+DCs.	Eur J Immunol. 2016 Aug;46(8):1867-77
C57BL/6 wild-type and iNOS-deficient bone marrow cells	10 mM	7 days	Α-GalCer suppressed eosinophil production in wild-type bone marrow but was ineffective in iNOS-deficient bone marrow	Br J Pharmacol. 2015 Jul;172(13):3313-25
BALB/c bone marrow cells	10-1000 mM	7 days	Α-GalCer suppressed IL-5-stimulated eosinopoiesis by inducing apoptosis	Br J Pharmacol. 2015 Jul;172(13):3313-25
Primary peritoneal macrophages	100 ng/mL	72 hours	To evaluate the effect of αGC on macrophage migration and collagen secretion. Results showed that αGC pretreatment significantly promoted macrophage migration and increased the secretion of collagen III, MCP-1, and MIP-1α.	Acta Pharmacol Sin. 2020 Nov;41(11):1416-1426
Splenocytes	100 ng/ml	72 hours	To evaluate the inhibitory effect of α-GalCer-activated splenocytes on Mtb replication. Results showed that α-GalCer significantly reduced CFU counts.	Am J Respir Crit Care Med. 2010 Sep 15;182(6):841-7
Peritoneal macrophages	100 ng/ml	72 hours	To evaluate the inhibitory effect of α-GalCer-activated iNKT cells on Mtb replication. Results showed that α-GalCer and IFN-γ had a cooperative effect on CFU control.	Am J Respir Crit Care Med. 2010 Sep 15;182(6):841-7

C57BL/6 mice	C57BL/6 mice under standard pathogen-free conditions	Intravenous injection	1 µg	Multiple injections, interval not specified	To test if nanoparticle formulated αGalCer can repeatedly stimulate NKT cells without inducing anergy. Results showed nanoparticle formulated αGalCer could repeatedly stimulate NKT cells to produce IFN-γ, while soluble form was only effective in the first injection.	Vaccine. 2009 May 26;27(25-26):3484-8
Mice	C57BL/6 and BALB/c mice	Oral	10 μg	Three immunizations on days 0 and 1; 14 and 15, and 28 and 29	To evaluate the ability of α-GalCer to enhance the immunogenicity of the Dukoral? vaccine. Results showed that α-GalCer significantly enhanced bacteria- and CTB-specific IgA and IgG1 responses in the intestine and serum.	Mucosal Immunol. 2019 Jul;12(4):1055-1064
BALB/c mice	4T1 metastatic breast cancer model	Intraperitoneal injection	100 ng	Three injections on days 14, 15, and 16 of treatment	To evaluate the efficacy of α-Galactosylceramide in combination with a Listeria-based vaccine against metastatic breast cancer. Results showed that the combination therapy significantly reduced the number of metastases, but α-Galactosylceramide alone was accompanied by severe liver toxicity.	Br J Cancer. 2014 Nov 11;111(10):1945-54
Pigs	Swine influenza model	Intramuscular injection	100 μg/kg	Two immunizations, 16 days apart	Evaluated the protective effect of α-GalCer as a vaccine adjuvant against swine influenza, showing significant reduction in viral replication and shedding	Sci Rep. 2016 Mar 23;6:23593
Mice	BALB/c and C57BL/6 wild-type and their mutants	Intraperitoneal injection	100 μg/kg	Single injection, 24 hours before sacrifice	Α-GalCer pretreatment in vivo suppressed colony formation by GM-CSF-stimulated bone marrow progenitors in semi-solid cultures	Br J Pharmacol. 2015 Jul;172(13):3313-25
Mice	Pulmonary tuberculosis infection model	Intraperitoneal or intratracheal injection	100 μg/kg or 500 μg/kg	Single or multiple doses, lasting 30 days	To evaluate the therapeutic effect of α-GalCer on pulmonary tuberculosis infection. Results showed that α-GalCer significantly prolonged the survival of infected mice and had a synergistic effect when combined with isoniazid.	Am J Respir Crit Care Med. 2010 Sep 15;182(6):841-7
C57BL/6J mice	Α-Galcer-induced NKT hepatitis model	Intravenous injection	150 μg/kg	Single dose, samples collected after 16 hours	To investigate α-Galcer-induced liver injury and its mechanisms, results showed that α-Galcer treatment increased serum ALT and AST levels, neutrophil and macrophage infiltration in the liver, and ROS production.	Hepatol Commun. 2025 Mar 24;9(4):e0592
C57BL/6 mice	LPS/D-GalN-induced sepsis model	Intraperitoneal injection	2 µg/mouse	Single administration, sepsis induced 7 days later	Α-GalCer pretreatment significantly attenuated LPS/D-GalN-induced septic lethality by polarizing iNKT cells towards IL4- and IL10-producing phenotypes and increasing IL10-producing B cells.	Front Immunol. 2024 Sep 17;15:1457690
BALB/c mice	OVA- or HDM-induced murine asthma model	Intraperitoneal injection	2 μg	Single injection, 1 day before the first sensitization	Α-GalCer treatment before allergen sensitization promotes iNKT cell–mediated induction of Treg cells, preventing Th2 cell responses in murine asthma models.	J Biol Chem. 2019 Apr 5;294(14):5438-5455
BALB/c mice	Wild-type and CD1d knockout mice	Intraperitoneal injection	2 μg	Single injection	To evaluate the effect of α-GalCer on the expansion of Treg cells in the lungs of mice. Results showed that intraperitoneal injection of α-GalCer promoted the expansion of Treg cells in WT mice but not in CD1d knockout mice. Additionally, α-GalCer induced the generation of Treg cells through IL-2 release by activated iNKT cells.	J Cell Mol Med. 2019 Feb;23(2):1072-1085
BALB/c mice	Wild-type and CD1d knockout mice	Intraperitoneal injection	2 μg	Single injection	To evaluate the effect of α-GalCer on the expansion of lung Treg cells, results showed that intraperitoneal injection of α-GalCer promoted the expansion of lung Treg cells in WT mice through the activation of iNKT cells, and this process was dependent on IL-2 production.	J Cell Mol Med. 2019 Feb;23(2):1072-1085
C57BL/6 mice	TC-1 tumor model	Intramuscular injection	2 μg	Two immunizations, one week apart	To evaluate the adjuvant effect of α-GalCer on DNA and DC vaccines	Vaccine. 2010 Oct 21;28(45):7297-305
Mice	Syngeneic-mated C57BL/6 mice and allogeneic-mated mice (C57BL/6 (♀)×BALB/c (♂))	Intraperitoneal injection	2 μg/mouse	Single injection on gestation day 7.5	To investigate the effect of α-GalCer on miscarriage in pregnant mice. The results showed that α-GalCer significantly increased the miscarriage rate when injected on gestation day 7.5, and this effect was not observed in iNKT cell-deficient Jα18 KO mice.	Eur J Immunol. 2016 Aug;46(8):1867-77
C57BL/6 mice	B16F10 melanoma model	Subcutaneous injection	20 ng	The first immunization occurred three days after tumor inoculation, and a booster dose was given ten days after.	To evaluate the anti-tumor efficacy of GalCer-loaded nano-vaccine in a melanoma model. Results showed that the NP[M+G+GalCer] group had the smallest tumor volume and induced significant infiltration of NK and NKT cells.	Acta Biomater. 2018 Aug;76:193-207
C57BL/6J mice	ISO-induced cardiac injury model	Intraperitoneal injection	3 μg/mouse	Every other day for a total of three times	To evaluate the effect of αGC on ISO-induced cardiac injury. Results showed that αGC significantly accelerated the progression of cardiac injury, leading to enhanced cardiac hypertrophy and fibrosis with prominent increases in collagen deposition and TGF-β1, IL-6, and α-SMA expression.	Acta Pharmacol Sin. 2020 Nov;41(11):1416-1426
C57BL/6 WT mice	Wild-type and Batf3KO mice	Intravenous injection	30 nM liposomal solution (containing 200 ng αGC and 150 ng OVA)	Single injection, observation time points included 2 hours, 16 hours, and 7 days post-injection	To evaluate the immune activation capacity of GM3-αGC-OVA liposomes in vivo, particularly CD8+ T cell and B cell responses. Results showed that GM3-αGC-OVA liposomes significantly enhanced antigen-specific CD8+ T cell and B cell responses.	Vaccines (Basel). 2021 Jan 16;9(1):56
Mice	B16-F10 melanoma model	Intravenous injection	4 nmol	Single injection, observed for 15 days	Evaluate the anti-tumor activity of AH10-7 in the B16-F10 melanoma model, showing that AH10-7 exhibited at least comparable anti-tumor activity to KRN7000 in both wild-type and hCD1d-KI mice	Cell Chem Biol. 2018 May 17;25(5):571-584. e8
C57BL/6 mice	Panc02 and TC-1 subcutaneous tumor models	Intraperitoneal injection	429 ng	Twice a week, throughout the study	To evaluate the antitumor activity of PLS-α-GalCer in vivo, results showed that PLS-α-GalCer significantly suppressed tumor growth, increased tumor-infiltrating T cells and NKT cells, and enhanced the M1/M2 macrophage ratio.	J Immunother Cancer. 2025 Mar 22;13(3):e009539
Mice	ApcMin/+ mouse model of colon cancer	Intraperitoneal injection	4μg	Once weekly for 3 weeks	Combined treatment with α-GalCer and PD-1 blockade significantly reduced polyp numbers in both the small intestine and colon of ApcMin/+ mice, prevented loss of iNKT cells, and promoted a shift towards an iNKT1 phenotype.	Front Immunol. 2020 Oct 20;11:581301
Mice	Adenine-induced tubule-interstitial nephritis	Intraperitoneal injection	5 μg	Single injection, duration of 10 days	To analyze the role of activated iNKT cells in the adenine-induced renal injury model. Results showed that αGalCer administration significantly reduced serum creatinine levels, proinflammatory cytokines, and renal fibrosis.	Mol Med. 2015 Jun 18;21(1):553-62
Humanized mice	HIS-CD8/NKT mice	Intramuscular	50 μg	Three immunizations with 2-week intervals	Induce a potent Melan-A-specific human CD8+ T cell response	Front Immunol. 2020 Aug 18;11:2043

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CAS No.: 158021-47-7

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CAS No.: 158021-47-7

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NCT00363155	Hepatitis B, Chronic	PHASE1\|PHASE2	COMPLETED	2025-07-06	Erasmus MC, University Medical... More >> Center Rotterdam, Rotterdam, 3015GD, Netherlands Less <<
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NCT00003985	Lung Cancer\|Unspecified Adult ... More >>Solid Tumor, Protocol Specific Less <<	PHASE1	WITHDRAWN	-	Innsbruck Universitaetsklinik,... More >> Innsbruck, A-6020, Austria\|Kaiser Franz Josef Hospital, Vienna, A-1100, Austria\|Institut Jules Bordet, Brussels, 1000, Belgium\|Ludwig Institute for Cancer Research-Brussels Branch, Brussels, B-1200, Belgium\|Universitair Ziekenhuis Antwerpen, Edegem, B-2650, Belgium\|U.Z. Gasthuisberg, Leuven, B-3000, Belgium\|Herlev Hospital - University Hospital of Copenhagen, Herlev, DK-2730, Denmark\|Centre Jean Perrin, Clermont-Ferrand, 63011, France\|Centre Leon Berard, Lyon, 69373, France\|CRLCC Nantes - Atlantique, Nantes-Saint Herblain, 44805, France\|Institut Claudius Regaud, Toulouse, 31052, France\|Institut Gustave Roussy, Villejuif, F-94805, France\|Universitaetsklinik und Strahlenklinik - Essen, Essen, D-45122, Germany\|Klinikum Nurnberg, Nuremberg (Nurnberg), D-90419, Germany\|Antoni van Leeuwenhoekhuis, Amsterdam, 1066 CX, Netherlands\|Academisch Ziekenhuis der Vrije Universiteit, Amsterdam, 1117 MB, Netherlands\|Academisch Ziekenhuis Groningen, Groningen, 9713 EZ, Netherlands\|University Medical Center Nijmegen, Nijmegen, NL-6252 HB, Netherlands\|Rotterdam Cancer Institute, Rotterdam, 3075 EA, Netherlands\|Norwegian Radium Hospital, Oslo, N-0310, Norway\|University Hospital, Basel, CH-4031, Switzerland\|Inselspital, Bern, Bern, CH-3010, Switzerland\|Kantonsspital - Saint Gallen, Saint Gallen, CH-9007, Switzerland\|Newcastle General Hospital, Newcastle Upon Tyne, England, NE4 6BE, United Kingdom\|Ninewells Hospital and Medical School, Dundee, Scotland, DD1 9SY, United Kingdom\|Western General Hospital, Edinburgh, Scotland, EH4 9NQ, United Kingdom\|C.R.C. Beatson Laboratories, Glasgow, Scotland, G61 1BD, United Kingdom Less <<

Precautionary Statements-General
Code	Phrase
P101	If medical advice is needed,have product container or label at hand.
P102	Keep out of reach of children.
P103	Read label before use
Prevention
Code	Phrase
P201	Obtain special instructions before use.
P202	Do not handle until all safety precautions have been read and understood.
P210	Keep away from heat/sparks/open flames/hot surfaces. - No smoking.
P211	Do not spray on an open flame or other ignition source.
P220	Keep/Store away from clothing/combustible materials.
P221	Take any precaution to avoid mixing with combustibles
P222	Do not allow contact with air.
P223	Keep away from any possible contact with water, because of violent reaction and possible flash fire.
P230	Keep wetted
P231	Handle under inert gas.
P232	Protect from moisture.
P233	Keep container tightly closed.
P234	Keep only in original container.
P235	Keep cool
P240	Ground/bond container and receiving equipment.
P241	Use explosion-proof electrical/ventilating/lighting/equipment.
P242	Use only non-sparking tools.
P243	Take precautionary measures against static discharge.
P244	Keep reduction valves free from grease and oil.
P250	Do not subject to grinding/shock/friction.
P251	Pressurized container: Do not pierce or burn, even after use.
P260	Do not breathe dust/fume/gas/mist/vapours/spray.
P261	Avoid breathing dust/fume/gas/mist/vapours/spray.
P262	Do not get in eyes, on skin, or on clothing.
P263	Avoid contact during pregnancy/while nursing.
P264	Wash hands thoroughly after handling.
P265	Wash skin thouroughly after handling.
P270	Do not eat, drink or smoke when using this product.
P271	Use only outdoors or in a well-ventilated area.
P272	Contaminated work clothing should not be allowed out of the workplace.
P273	Avoid release to the environment.
P280	Wear protective gloves/protective clothing/eye protection/face protection.
P281	Use personal protective equipment as required.
P282	Wear cold insulating gloves/face shield/eye protection.
P283	Wear fire/flame resistant/retardant clothing.
P284	Wear respiratory protection.
P285	In case of inadequate ventilation wear respiratory protection.
P231 + P232	Handle under inert gas. Protect from moisture.
P235 + P410	Keep cool. Protect from sunlight.
Response
Code	Phrase
P301	IF SWALLOWED:
P304	IF INHALED:
P305	IF IN EYES:
P306	IF ON CLOTHING:
P307	IF exposed:
P308	IF exposed or concerned:
P309	IF exposed or if you feel unwell:
P310	Immediately call a POISON CENTER or doctor/physician.
P311	Call a POISON CENTER or doctor/physician.
P312	Call a POISON CENTER or doctor/physician if you feel unwell.
P313	Get medical advice/attention.
P314	Get medical advice/attention if you feel unwell.
P315	Get immediate medical advice/attention.
P320
P302 + P352	IF ON SKIN: wash with plenty of soap and water.
P321
P322
P330	Rinse mouth.
P331	Do NOT induce vomiting.
P332	IF SKIN irritation occurs:
P333	If skin irritation or rash occurs:
P334	Immerse in cool water/wrap n wet bandages.
P335	Brush off loose particles from skin.
P336	Thaw frosted parts with lukewarm water. Do not rub affected area.
P337	If eye irritation persists:
P338	Remove contact lenses, if present and easy to do. Continue rinsing.
P340	Remove victim to fresh air and keep at rest in a position comfortable for breathing.
P341	If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.
P342	If experiencing respiratory symptoms:
P350	Gently wash with plenty of soap and water.
P351	Rinse cautiously with water for several minutes.
P352	Wash with plenty of soap and water.
P353	Rinse skin with water/shower.
P360	Rinse immediately contaminated clothing and skin with plenty of water before removing clothes.
P361	Remove/Take off immediately all contaminated clothing.
P362	Take off contaminated clothing and wash before reuse.
P363	Wash contaminated clothing before reuse.
P370	In case of fire:
P371	In case of major fire and large quantities:
P372	Explosion risk in case of fire.
P373	DO NOT fight fire when fire reaches explosives.
P374	Fight fire with normal precautions from a reasonable distance.
P376	Stop leak if safe to do so. Oxidising gases (section 2.4) 1
P377	Leaking gas fire: Do not extinguish, unless leak can be stopped safely.
P378
P380	Evacuate area.
P381	Eliminate all ignition sources if safe to do so.
P390	Absorb spillage to prevent material damage.
P391	Collect spillage. Hazardous to the aquatic environment
P301 + P310	IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P301 + P312	IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P301 + P330 + P331	IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.
P302 + P334	IF ON SKIN: Immerse in cool water/wrap in wet bandages.
P302 + P350	IF ON SKIN: Gently wash with plenty of soap and water.
P303 + P361 + P353	IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.
P304 + P312	IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell.
P304 + P340	IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P304 + P341	IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.
P305 + P351 + P338	IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing.
P306 + P360	IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes.
P307 + P311	IF exposed: call a POISON CENTER or doctor/physician.
P308 + P313	IF exposed or concerned: Get medical advice/attention.
P309 + P311	IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician.
P332 + P313	IF SKIN irritation occurs: Get medical advice/attention.
P333 + P313	IF SKIN irritation or rash occurs: Get medical advice/attention.
P335 + P334	Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages.
P337 + P313	IF eye irritation persists: Get medical advice/attention.
P342 + P311	IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician.
P370 + P376	In case of fire: Stop leak if safe to Do so.
P370 + P378	In case of fire:
P370 + P380	In case of fire: Evacuate area.
P370 + P380 + P375	In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion.
P371 + P380 + P375	In case of major fire and large quantities: Evacuate area. Fight fire remotely due to the risk of explosion.
Storage
Code	Phrase
P401
P402	Store in a dry place.
P403	Store in a well-ventilated place.
P404	Store in a closed container.
P405	Store locked up.
P406	Store in corrosive resistant/ container with a resistant inner liner.
P407	Maintain air gap between stacks/pallets.
P410	Protect from sunlight.
P411
P412	Do not expose to temperatures exceeding 50 oC/ 122 oF.
P413
P420	Store away from other materials.
P422
P402 + P404	Store in a dry place. Store in a closed container.
P403 + P233	Store in a well-ventilated place. Keep container tightly closed.
P403 + P235	Store in a well-ventilated place. Keep cool.
P410 + P403	Protect from sunlight. Store in a well-ventilated place.
P410 + P412	Protect from sunlight. Do not expose to temperatures exceeding 50 oC/122oF.
P411 + P235	Keep cool.
Disposal
Code	Phrase
P501	Dispose of contents/container to ...
P502	Refer to manufacturer/supplier for information on recovery/recycling

Physical hazards
Code	Phrase
H200	Unstable explosive
H201	Explosive; mass explosion hazard
H202	Explosive; severe projection hazard
H203	Explosive; fire, blast or projection hazard
H204	Fire or projection hazard
H205	May mass explode in fire
H220	Extremely flammable gas
H221	Flammable gas
H222	Extremely flammable aerosol
H223	Flammable aerosol
H224	Extremely flammable liquid and vapour
H225	Highly flammable liquid and vapour
H226	Flammable liquid and vapour
H227	Combustible liquid
H228	Flammable solid
H229	Pressurized container: may burst if heated
H230	May react explosively even in the absence of air
H231	May react explosively even in the absence of air at elevated pressure and/or temperature
H240	Heating may cause an explosion
H241	Heating may cause a fire or explosion
H242	Heating may cause a fire
H250	Catches fire spontaneously if exposed to air
H251	Self-heating; may catch fire
H252	Self-heating in large quantities; may catch fire
H260	In contact with water releases flammable gases which may ignite spontaneously
H261	In contact with water releases flammable gas
H270	May cause or intensify fire; oxidizer
H271	May cause fire or explosion; strong oxidizer
H272	May intensify fire; oxidizer
H280	Contains gas under pressure; may explode if heated
H281	Contains refrigerated gas; may cause cryogenic burns or injury
H290	May be corrosive to metals
Health hazards
Code	Phrase
H300	Fatal if swallowed
H301	Toxic if swallowed
H302	Harmful if swallowed
H303	May be harmful if swallowed