Mizoribine
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Mizoribine
structure -
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CAS No:
50924-49-7
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Formula:
C9H13N3O6
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Chemical Name:
Mizoribine
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Synonyms:
1H-Imidazole-4-carboxamide,5-hydroxy-1-β-D-ribofuranosyl-;5-Hydroxy-1-β-D-ribofuranosyl-1H-imidazole-4-carboxamide;Bredinin;Mizoribine;β-Bredinin;HE 69;NSC 289637;55727-07-6
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Categories:
Active Pharmaceutical Ingredients > Drugs Influencing Immune Function
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CAS No:
Description
Mizoribine(NSC 289637; HE 69; β-Bredinin) is an immunosuppressive agents (IC50=100 uM) that inhibit the proliferation of lymphocytes selectively, via inhibition of IMPDH.IC50 Value:Target: IMPDHin vitro: Unlike azathioprine, Mizoribine is not taken up by nucleic acids in the cell. Instead, after phosphorylation MZR-5 -monophosphate inhibits GMP synthesis by the antagonistic blocking of IMPDH (Ki = 10(-8)M) and GMP- synthetase (Ki =10(-5) M) [1]. Pretreatment of cells with MZR partially,
Mizoribine is a member of imidazoles. It has a role as an anticoronaviral agent.|Mizoribine has been investigated for the treatment of Rheumatoid Arthritis.
Characteristics
151
-1.9
white to off-white crystalline powder
2.1±0.1 g/cm3
>200 °C (decomp)
755.9ºC at 760 mmHg
410.9±32.9 °C
1.795
2-8°C
Oral-rat LD50: 3100 mg/kg; Abdominal cavity-mouse LD50: 5000 mg/kg
Thermal decomposition to release toxic nitrogen oxide gas
D27 -35° (c = 0.8 in H2O)
Safety Information
NONH for all modes of transport
3
46-60-61-36/37/38
53-22-26-36/37/39-45
NI3980000
T
Treasury ventilation, low temperature, dry
Stable at normal temperatures and pressures.
P201-P261-P305 + P351 + P338-P308 + P313
H315-H319-H335-H360
|Danger|H315 (100%): Causes skin irritation [Warning Skin corrosion/irritation]|P201, P202, P261, P264, P271, P280, P281, P302+P352, P304+P340, P305+P351+P338, P308+P313, P312, P321, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 39 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
Drug Information
Chemical substances, produced by microorganisms, inhibiting or preventing the proliferation of neoplasms. (See all compounds classified as Antibiotics, Antineoplastic.)|Agents used in the treatment of malaria. They are usually classified on the basis of their action against plasmodia at different stages in their life cycle in the human. (From AMA, Drug Evaluations Annual, 1992, p1585) (See all compounds classified as Antimalarials.)|Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. (See all compounds classified as Enzyme Inhibitors.)|Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions.They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects. (See all compounds classified as Anti-Inflammatory Agents, Non-Steroidal.)|Agents that suppress immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-CELLS or by inhibiting the activation of HELPER CELLS. While immunosuppression has been brought about in the past primarily to prevent rejection of transplanted organs, new applications involving mediation of the effects of INTERLEUKINS and other CYTOKINES are emerging. (See all compounds classified as Immunosuppressive Agents.)|Substances that inhibit the growth or reproduction of BACTERIA. (See all compounds classified as Anti-Bacterial Agents.)
bredinin
Computed Properties
Molecular Weight:259.22
XLogP3:-1.9
Hydrogen Bond Donor Count:5
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:3
Exact Mass:259.08043514
Monoisotopic Mass:259.08043514
Topological Polar Surface Area:151
Heavy Atom Count:18
Complexity:329
Defined Atom Stereocenter Count:4
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes
Drug Function and Efficacy
This drug has an immunosuppressive effect and can inhibit the proliferation of lymphoid system cells; inhibit the blastogenesis reaction caused by various mitosis; inhibit the production of antibodies in primary and secondary responses; prolong the survival time of transplanted kidneys in dogs; competitively inhibit the inosine to guanylate pathway in the purine synthesis system and inhibit nucleic acid synthesis, but it is not taken up into high-molecular nucleic acids (in vitro).
Registered Holders
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PHARMACOSTECH CO.,LTD.
Active
South Korea
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North China Pharmaceutical Huasheng Co., Ltd.
Active
China
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Nanjing Hicin Pharmaceutical Co., Ltd.
Active
China
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