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CAS No. :	263707-16-0
Formula :	C₁₆H₁₅ClN₄O₂
M.W :	330.77
SMILES Code :	O=C(C1=NOC(C(C)(C)C)=C1)/C(C#N)=N/NC2=CC(Cl)=CC=C2
MDL No. :	N/A
InChI Key :	DXEATJQGQHDURZ-DEDYPNTBSA-N
Pubchem ID :	6077765

GHS Pictogram:
Signal Word:	Warning
Hazard Statements:	H302-H315-H319-H335
Precautionary Statements:	P261-P305+P351+P338

Description	ESI-09 is a novel noncyclic nucleotide EPAC antagonist, showcasing selective inhibitory properties with IC50 values of 3.2 μM for EPAC1 and 1.4 μM for EPAC2, underscoring its potential in targeting these exchange proteins directly activated by cAMP[1].
Target	EPAC1 EPAC1, IC50:3.2 μM EPAC2 EPAC2, IC50:1.4 μM

Rat urothelium-denuded detrusor strips	10 µM	15 minutes	ESI-09 prevented isoprenaline-induced adenosine release from rat detrusor strips, indicating the role of EPAC1 in β3-adrenoceptor-induced adenosine release.	Br J Pharmacol. 2020 Apr;177(7):1589-1608.
Human urothelium-denuded detrusor strips	10 µM	15 minutes	ESI-09 prevented mirabegron- and isoprenaline-induced adenosine release from human detrusor strips, indicating the role of EPAC1 in β3-adrenoceptor-induced adenosine release.	Br J Pharmacol. 2020 Apr;177(7):1589-1608.
Mouse airway smooth muscle cells (ASMCs)	1, 10, 100 µM	24, 48, 72 hours	ESI-09 promoted ASMCs proliferation at 10 and 100 μM	Respir Res. 2019 Dec 18;20(1):285.
Human umbilical vein endothelial cells (HUVECs)	5 µM	30 minutes	To evaluate the effect of ESI-09 on the attachment and invasion of Rickettsia australis into HUVECs. Results showed that ESI-09 significantly reduced intracellular and total bacterial counts.	Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19615-20.
Mouse airway smooth muscle cells (ASMCs)	1, 10, 100 µM	30 minutes	ESI-09 promoted SOCE in ASMCs at 10 and 100 μM	Respir Res. 2019 Dec 18;20(1):285.
Left atrial fibroblasts	1 µM	48 hours	To evaluate the effect of Epac1 inhibition on isoproterenol's effect. ESI-09 blocked the isoproterenol-induced decrease in collagen protein expression.	Cardiovasc Res. 2019 Jan 1;115(1):94-106.
Left atrial fibroblasts	1 µM	48 hours	To evaluate the effect of Epac1 inhibition on collagen expression. ESI-09 increased COL1A1 mRNA levels by 40% and collagen I protein expression by 97%.	Cardiovasc Res. 2019 Jan 1;115(1):94-106.
A549 cells	2 µM	48 hours	Evaluate the effect of ESI-09 on lung cancer cell survival under low-glucose conditions, results showed ESI-09 significantly reduced cell survival	Mol Metab. 2020 Dec;42:101093.
Mouse airway smooth muscle cells (ASMCs)	1, 10, 100 µM	48 hours	ESI-09 had no significant effect on ASMCs apoptosis	Respir Res. 2019 Dec 18;20(1):285.
PC3 cells	2 µM	72 hours	Evaluate the effect of ESI-09 on lung cancer cell survival under low-glucose conditions, results showed ESI-09 significantly reduced cell survival	Mol Metab. 2020 Dec;42:101093.
H1975 cells	2 µM	72 hours	Evaluate the effect of ESI-09 on lung cancer cell survival under low-glucose conditions, results showed ESI-09 significantly reduced cell survival	Mol Metab. 2020 Dec;42:101093.
H1299 cells	2 µM	72 hours	Evaluate the effect of ESI-09 on lung cancer cell survival under low-glucose conditions, results showed ESI-09 significantly reduced cell survival	Mol Metab. 2020 Dec;42:101093.
MCF-7 breast cancer cells	1 µM	72 hours	ESI-09, as an EPAC inhibitor, abrogated the isoprenaline-induced lipid droplet accumulation	Int J Mol Sci. 2023 Jan 1;24(1):767.
Human atrial myocytes	10 µM		ESI-09, as an Epac inhibitor, reversed or prevented the noradrenaline-induced up-regulation of ICl.vol under hypotonic conditions	Br J Pharmacol. 2018 Aug;175(16):3422-3432.

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CAS No.: 263707-16-0

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CAS No.: 263707-16-0

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Rats	Neonatal colorectal distension (CRD)-induced visceral hypersensitivity model	Intra-PVN microinjection	1.0 μg/μl	Single injection, needle retained for 10 minutes	Inhibition of Epac1 increased the firing frequency of PVN CRF neurons, facilitated visceral hypersensitivity and pain precipitation	CNS Neurosci Ther. 2022 Sep;28(9):1393-1408
Female BALB/c mice	Acute and chronic asthma models	Intraperitoneal injection	10 mg/kg	30 min before each OVA challenge for 3 days (acute) or 6 weeks (chronic)	ESI-09 aggravated airway inflammation and airway remodeling	Respir Res. 2019 Dec 18;20(1):285.
Mice	Orthotopic metastatic PDA mouse model	Intraperitoneal injection	10 mg/kg	3 weeks	Reduced local and distant spread of MIA PaCa-2 cells and significantly decreased metastasis to the liver	J Med Chem. 2015 Aug 13;58(15):6033-47
Mice (C57BL/6)	Fatal spotted fever group (SFG) rickettsiosis model	Intraperitoneal injection	10 mg/kg/day	Once daily for 5 days before infection and 7 days after infection	To evaluate the therapeutic effect of ESI-09 on fatal SFG rickettsiosis. Results showed that ESI-09 significantly improved survival and reduced pathological damage.	Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19615-20.
Mice	Epac WT, Epac1–/–, Epac2–/–, and Epac1&2–/– mice	Intraperitoneal injection	10 mg/kg	Daily injections for 7 days	To investigate the effect of ESI-09 on urinary sodium excretion in mice, results showed that ESI-09 significantly increased urinary sodium excretion under a low-sodium diet, indicating its inhibitory effect on ENaC activity.	JCI Insight. 2022 Feb 8;7(3):e145653
Rat	Urethane-anaesthetized rats	Intravesical instillation	10 μM	Single administration	Pre-treatment with ESI-09 prevented the reduction of the voiding frequency caused by isoprenaline and forskolin, indicating the role of EPAC1 in β3-adrenoceptor-induced bladder function regulation.	Br J Pharmacol. 2020 Apr;177(7):1589-1608.
BALB/c-nu (nu/nu) mice	A549 cell xenograft model	Intraperitoneal injection	2 mg/kg or 10 mg/kg	Once daily for 21 days	Evaluate the inhibitory effect of ESI-09 on tumor growth, results showed ESI-09 significantly inhibited tumor growth and reduced tumor volume	Mol Metab. 2020 Dec;42:101093.
C57Bl/6 mice	GDNF-induced hyperalgesic priming model	Oral	20 mg/kg	Administered on the 13th and 14th day	ESI-09 significantly reduced the duration of PGE2 hyperalgesia in GDNF-primed mice.	Front Pharmacol. 2018 Jun 5;9:592
C57BL/6 mice	Myocardial infarction model	Intraperitoneal injection	20 mg/kg/day	Once daily for 5 days	To evaluate the effect of Epac1 inhibition post-MI. ESI-09 did not significantly alter the heart weight to body weight ratio, LV function, or atrial fibrosis.	Cardiovasc Res. 2019 Jan 1;115(1):94-106.
Rats	Chronic morphine-induced analgesic tolerance model	Intrathecal injection	5 μg	Once daily for 7 days	ESI-09 significantly attenuated the development of morphine-induced anti-nociceptive tolerance while retaining the anti-nociceptive effect of morphine. Additionally, ESI-09 reduced the phosphorylation of PKC ε and up-regulated expression of Epac after chronic morphine exposure.	Br J Pharmacol. 2018 May;175(10):1760-1769
Mice	CFA-induced inflammatory mechanical hyperalgesia model	Oral	5, 20, or 50 mg/kg	Treatment started on the third day after CFA administration	To evaluate the inhibitory effect of ESI-09 on established CFA-induced mechanical hyperalgesia	Proc Natl Acad Sci U S A. 2016 Mar 15;113(11):3036-41

Bio Calculators
Preparing Stock Solutions		1mg	5mg	10mg
Preparing Stock Solutions	1 mM 5 mM 10 mM	3.02mL 0.60mL 0.30mL	15.12mL 3.02mL 1.51mL	30.23mL 6.05mL 3.02mL
Dissolving Methods	Animal experiment Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn: in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day; The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound. Protocol 1 Protocol 2

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