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Chemical Structure| 50924-49-7 Chemical Structure| 50924-49-7

Structure of Mizoribine
CAS No.: 50924-49-7

Chemical Structure| 50924-49-7

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Mizoribine is an immunosuppressive agents (IC50=100 μM) that inhibit the proliferation of lymphocytes selectively, via inhibition of IMPDH.

Synonyms: NSC 289637; HE 69; Bredinin

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Product Details of Mizoribine

CAS No. :50924-49-7
Formula : C9H13N3O6
M.W : 259.22
SMILES Code : O=C(C1=C(O)N([C@H]2[C@@H]([C@@H]([C@@H](CO)O2)O)O)C=N1)N
Synonyms :
NSC 289637; HE 69; Bredinin
MDL No. :MFCD00057221
InChI Key :HZQDCMWJEBCWBR-UUOKFMHZSA-N
Pubchem ID :104762

Safety of Mizoribine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P280-P305+P351+P338-P310

Related Pathways of Mizoribine

DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human peripheral blood T cells 1-50 µg/ml 72 h Mizoribine was able to inhibit T cell proliferation in a dose-dependent manner, with inhibition rates ranging from 10-100%. HPLC measurements showed that mizoribine led to a decrease in intracellular GTP levels, and that repletion of GTP reversed its antiproliferative effects. PMC329885
Vero E6 cells 10 µg/ml 20 h Mizoribine inhibited the replication of SARS-CoV more strongly than ribavirin in yield reduction assay. PMC7114120
Vero 76 cells >40 µM Evaluate the in vitro inhibitory effect of Mizoribine on SARS-CoV, results showed no significant inhibition at tested concentrations. PMC7114261

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Lewis rats Hamster-to-rat heart xenotransplantation model Oral 7.5 mg/kg Daily for 5 days As an adjunct to FK506, mizoribine showed intermediate efficacy in prolonging heart xenograft survival PMC2957097
BALB/c mice SARS-CoV infection model Intraperitoneal injection 25 mg/kg Twice daily for 3 days Evaluate the in vivo inhibitory effect of Mizoribine on SARS-CoV infection, results showed Mizoribine had no significant inhibitory effect on viral replication. PMC7114261
Rats ACI-LEW heterotopic heart transplantation model Gastric instillation 2.5, 5, 10 mg/kg Once daily for 14 days Mizoribine in combination with low-dose FK506 showed significant therapeutic synergism, particularly at the lowest dose of 2.5 mg/kg, significantly prolonging median graft survival from 15 days to 26 days PMC2953379

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02256150 Lupus Nephritis Phase 3 Active, not recruiting March 2019 -
NCT02257697 Nephrotic Syndrome Phase 3 Active, not recruiting November 2018 -
NCT02373202 - Completed - -
NCT02005757 Rheumatoid Arthritis Phase 2 Unknown October 2016 Korea, Republic of ... More >> Hallym University Sacred Heart Hospital Recruiting Anyang, Korea, Republic of Contact: Young-Il Seo, PhD       yiseo@hallym.or.kr    Principal Investigator: Young-Il Seo, PhD          Hallym University chuncheon Sacred Heart Hospital Recruiting Chuncheon, Korea, Republic of Contact: Kyeong Min Son, PhD       jollyfox@hanmail.net    Principal Investigator: Kyeong Min Son          Eulji University Hospital Recruiting Daejeon, Korea, Republic of Contact: Donghyuk Sheen, PhD       rheuma@eulji.ac.kr    Principal Investigator: Donghyuk Sheen, PhD          Gangneung Asan Hospital Recruiting Gangneung, Korea, Republic of Contact: Sung-Soo Kim, Ph.D    82-33-610-3061    drkiss@ulsan.ac.kr    Principal Investigator: Sung-Soo Kim, Ph.D          Kangwon National University Hospital Recruiting Kangwon, Korea, Republic of Contact: Kiwon Moon, PhD       kiwonmoon@kangwon.ac.kr    Principal Investigator: Kiwon Moon          Kyung Hee University hospital Recruiting Seoul, Korea, Republic of Contact: Seung-Jae Hong, phD       hsj718@khu.ac.kr    Principal Investigator: Seung-Jae Hong, phD          Soon Chun Hyang University Hospital Recruiting Seoul, Korea, Republic of Contact: Hyun-sook Kim, PhD       healthyra@schmc.ac.kr    Principal Investigator: Hyunsook Kim Less <<
NCT02373202 Rheumatoid Arthritis Phase 3 Completed - Japan ... More >> Investigational Site Number 392010 Asahi-Shi, Japan Investigational Site Number 392001 Asahikawa-Shi, Japan Investigational Site Number 392070 Beppu-Shi, Japan Investigational Site Number 392036 Chiba-Shi, Japan Investigational Site Number 392083 Chuo-Ku, Japan Investigational Site Number 392004 Fukui-Shi, Japan Investigational Site Number 392039 Fukuoka-Shi, Japan Investigational Site Number 392030 Ichinomiya-Shi, Japan Investigational Site Number 392002 Iizuka-Shi, Japan Investigational Site Number 392019 Kagoshima-Shi, Japan Investigational Site Number 392066 Kamakura-Shi, Japan Investigational Site Number 392050 Kato-Shi, Japan Investigational Site Number 392037 Kawachi-Nagano-Shi, Japan Investigational Site Number 392099 Kawasaki-Shi, Japan Investigational Site Number 392013 Kitakyushu-Shi, Japan Investigational Site Number 392097 Kochi-Shi, Japan Investigational Site Number 392065 Kushiro-Shi, Japan Investigational Site Number 392026 Matsuyama-Shi, Japan Investigational Site Number 392034 Miyagi-Gun, Japan Investigational Site Number 392076 Nagoya-Shi, Japan Investigational Site Number 392080 Nagoya-Shi, Japan Investigational Site Number 392046 Narashino-Shi, Japan Investigational Site Number 392059 Oita-Shi, Japan Investigational Site Number 392062 Okayama-Shi, Japan Investigational Site Number 392027 Osaki-Shi, Japan Investigational Site Number 392049 Sagamihara-Shi, Japan Investigational Site Number 392014 Sapporo-Shi, Japan Investigational Site Number 392041 Sapporo-Shi, Japan Investigational Site Number 392073 Sapporo-Shi, Japan Investigational Site Number 392006 Sasebo-Shi, Japan Investigational Site Number 392021 Sendai-Shi, Japan Investigational Site Number 392022 Sendai-Shi, Japan Investigational Site Number 392033 Sendai-Shi, Japan Investigational Site Number 392071 Sendai-Shi, Japan Investigational Site Number 392029 Shizuoka-Shi, Japan Investigational Site Number 392023 Takaoka-Shi, Japan Investigational Site Number 392003 Tomakomai-Shi, Japan Investigational Site Number 392074 Urasoe-Shi, Japan Investigational Site Number 392079 Urayasu-Shi, Japan Investigational Site Number 392048 Yokohama-Shi, Japan Less <<
NCT05293704 Kidney Transplant Recipients|B... More >>K Virus Less << PHASE4 UNKNOWN 2024-05-01 The First Affiliated Hospital ... More >>of Sun Yat-sen University, Guangzhou, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.86mL

0.77mL

0.39mL

19.29mL

3.86mL

1.93mL

38.58mL

7.72mL

3.86mL

Dissolving Methods
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

References

 

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