Structure of Mizoribine
CAS No.: 50924-49-7
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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
4.5
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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 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H332-H335 |
Precautionary Statements: | P280-P305+P351+P338-P310 |
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 << |
Tags: Mizoribine | NSC 289637 | HE 69 | NSC289637 | NSC-289637 | HE69 | HE 69 | HE-69 | HCV | SARS-CoV | Antibiotic | Parasite | Hepatitis C virus | SARS coronavirus | nucleoside | Immunosuppressant | IMPDH | HCV RNA replication | IMPDH inhibitor | 50924-49-7
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H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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