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My CartCAS：3978-86-7
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 3978-86-7 |
| Name | Azatadine dimaleate |
| Molecular Formula | C20H22N2·2C4H4O4 |
| Molecular Weight | 522.55 |
| Solubility | Soluble in Water/DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| Delivery Time | 1-2 Days |
| EC | EINECS 223-615-8 |
| MDL | MFCD00242593 |
| SMILES | O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O.CN1CC/C(CC1)=C2C3=CC=CC=C3CCC4=CC=CN=C4\2 |
| InChIKey | SGHXFFAHXTZRQM-SPIKMXEPSA-N |
| InChI | InChI=1S/C20H22N2.2C4H4O4/c1-22-13-10-16(11-14-22)19-18-7-3-2-5-15(18)8-9-17-6-4-12-21-20(17)19;2*5-3(6)1-2-4(7)8/h2-7,12H,8-11,13-14H2,1H3;2*1-2H,(H,5,6)(H,7,8)/b;2*2-1- |
| PubChem CID | 5281066 |
| Target Point | Histamine Receptor |
| Passage | GPCR & G Protein;Neuronal Signaling;Immunology & Inflammation |
| Background | It is a histamine receptor and choline receptor inhibitor. |
| Biological Activity | Azatadine (SCH10649) 是一种抗组胺和抗胆碱能药物，IC50分别为6.5nM和10nM。[1] |
| IC50 | Histamine receptor: 6.5nM;Cholinergic :10nM[1] |
| In Vivo | Azatadine delays the onset of dyspnea-induced by aerosolized histamine，acetylcholine and serotonin in the conscious guinea-pig with PD50 of 0.01 mg/kg，0.739 mg/kg and 0.86 mg/kg. Azatadine protects conscious guinea-pigs against death induced by the intravenous injection of histamine with oral PD50 of 0.009 mg/kg in guinea-pig and 0.22 mg/kg in mice. [1] Following a single oral dose of Azatadine(4 mg)in fasted volunteers，a Cmax of 3 μg/L has been measured by RIA 4.2 hours after administration. Azatadine is almost completely metabolised by hydroxylation，demethylation and formation of zwitterion isomers by oxidative ring opening. Azatadine(8.8 mg oral)in healthy volunteers results in a Csub>max of 5.9 μg/L at 5.3 hours after treatment and bioavailability of 80%. [2] Azatadine(1 mg twice daily for 14 days)is effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis. [3] |
| Data Literature Source | [1] Tozzi S，et al. Agents Actions，1974，4(4)，264-270. [2] Simons FE，et al. Clin Pharmacokinet，1991，21(5)，372-393. [3] Katelaris C，et al. Asian Pac J Allergy Immunol，1990，8(2)，103-107 |
| Unit | Piece |
| Specification | 10mg 50mg |
是组胺受体和胆碱受体抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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