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My CartCAS：500287-72-9
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 500287-72-9 |
| Name | Rilpivirine |
| Molecular Formula | C22H18N6 |
| Molecular Weight | 366.42 |
| Solubility | Soluble in DMSO ≥5mg/mL |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD11046372 |
| SMILES | CC1=CC(=CC(=C1NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C)C=CC#N |
| InChIKey | YIBOMRUWOWDFLG-ONEGZZNKSA-N |
| InChI | InChI=1S/C22H18N6/c1-15-12-18(4-3-10-23)13-16(2)21(15)27-20-9-11-25-22(28-20)26-19-7-5-17(14-24)6-8-19/h3-9，11-13H，1-2H3，(H2，25，26，27，28)/b4-3+ |
| PubChem CID | 6451164 |
| Target Point | Reverse Transcriptase;HIV |
| Passage | Anti-infection |
| Background | It is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI) with high anti-HIV activity. |
| Biological Activity | Rilpivirine 是一种有效和特异性的二芳基嘧啶 (DAPY) 非核苷逆转录酶抑制剂 (NNRTI)，对野生型 HIV (EC50=0.4 nM) 和突变体 (EC50=0.1-2.0 nM) 具有很高的抗病毒活性，被用于治疗HIV-1感染。[1-2] |
| In Vitro | 利匹韦林对野生型 HIV-1(EC50=0.4 nM)和所有测试过的单突变体和双突变体(EC50=0.1-2.0 nM)都有活性。利匹韦林(10-5000 nM；30 d)在 1 μM 的浓度下，30 天内观察不到野生型 HIV-1 突破的迹象。利匹韦林对 81% 的临床分离株(约 1200 株重组临床分离株)的抑制浓度(EC50)小于 1 nM，对 94% 的临床分离株的抑制浓度(EC50)小于 10 nM。[1]在 MT4 T 细胞中，利匹韦林对野生型 HIV-1 M 组分离株的 EC50 值为亚纳摩尔(0.07-1.01 nM)，对 O 组分离株的 EC50 值为纳摩尔(2.88-8.45 nM)。[2] |
| In Vivo | 利匹韦林(10-160 毫克/千克；口服，1 个月)不会对大鼠产生异常影响，只是在较高剂量水平下会导致肝脏重量增加和特定物种甲状腺肥大。利匹韦林(静脉注射)的消除半衰期从大鼠的 4.4 小时到狗的 31 小时不等，大鼠的暴露量(AUCinf)为 3.1 μg-h/mL(4 毫克/千克)，狗为 8.7 μg-h/mL(1.25 毫克/千克)，猴为 1.4 μg-h/mL(1.25 毫克/千克)，兔为 44-μg h/mL(1.25 毫克/千克)。利匹韦林(口服)在大鼠和狗体内的半衰期分别为 2.8 小时和 39 小时，在大鼠和狗体内的口服生物利用度分别为 32% 和 31%[1]。 |
| Data Literature Source | [1]. Janssen PA，et al. In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2，6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474，rilpivirine). J Med Chem. 2005 Mar 24;48(6):1901-9. [2].Azijn H，et al. TMC278，a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI)，active against wild-type and NNRTI-resistant HIV-1. Antimicrob Agents Chemother. 2010 Feb;54(2):718-27. |
| Unit | Bottle |
| Specification | 5mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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