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[CAS NO. 599179-03-0] Vicrivirocmaleate
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-17377 |
| Brand: | MCE |
| CAS: | 599179-03-0 |
Overview
| MDL | MFCD09833218 |
|---|---|
| Molecular Weight | 649.70 |
| Molecular Formula | C32H42F3N5O6 |
| SMILES | CC1(N2C[C@H](C)N([C@H](C3=CC=C(C(F)(F)F)C=C3)COC)CC2)CCN(C(C4=C(C)N=CN=C4C)=O)CC1.O=C(O)/C=C\C(O)=O |
Summary
IC50 & Target
|
CCR5 2.5 nM (Ki) |
HIV-1 (301657) 1.8 nM (IC90, in PBMC cells) |
HIV-1 (ADA-M) 2.8 nM (IC90, in PBMC cells) |
HIV-1 (JrFL) 3.3 nM (IC90, in PBMC cells) |
||
|
HIV-1 (JV1083) 4.9 nM (IC90, in PBMC cells) |
HIV-1 (RU 570) 10 nM (IC90, in PBMC cells) |
||||
In Vitro
Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective and oral bioavailable inhibitor of CCR5, with a K i of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC 90 s of 3.3 (JrFL), 2.8 (ADA-M), 1.8 (301657), 4.9 (JV1083) and 10 nM (RU 570). In addition, Vicriviroc maleate shows a mean IC 50 and IC 90 of 0.45 nM and 4 nM for a panel of HIV isolates, and has weak activity against hERG activity (IC 50 , 5.8 μM) [1] . Vicriviroc maleate inhibits chemotactic response to MIP-1α with IC 50 values below 1 nM, and suppresses RANTES-induced signaling with a mean IC 50 of 4.2 ± 1.3 nM. Vicriviroc maleate potently suppresses all the viral isolates tested, with geometric mean EC 50 s of 0.04-2.3 nM and IC 90 s of 0.45-18 nM [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate; 10 mg/kg) has good oral availablity in rats and monkeys, with no acute CNS or GI effects in rats [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00551018 | Merck Sharp & Dohme LLC |
HIV Infections
|
December 2007 | Phase 2 |
| NCT00766597 | National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) |
HIV Infections
|
August 2009 | Phase 1|Phase 2 |
| NCT00686829 | Merck Sharp & Dohme LLC |
HIV|HIV Infections
|
June 30, 2005 | Phase 2 |
| NCT02356302 | National Institute of Allergy and Infectious Diseases (NIAID) |
HIV Infections
|
May 2015 | Phase 1 |
| NCT00243230 | Merck Sharp & Dohme LLC |
HIV Infections
|
September 19, 2005 | Phase 2 |
| NCT00632073 | Merck Sharp & Dohme LLC |
HIV Infections
|
March 2008 | Phase 1 |
| NCT00705419 | Merck Sharp & Dohme LLC |
HIV Infections
|
July 2007 | |
| NCT00551330 | Merck Sharp & Dohme LLC |
HIV Infections|Acquired Immunodeficiency Syndrome
|
September 2007 | Phase 2 |
| NCT00474370 | Merck Sharp & Dohme LLC |
HIV Infections|Acquired Immunodeficiency Syndrome
|
May 15, 2007 | Phase 3 |
| NCT00523211 | Merck Sharp & Dohme LLC |
HIV Infections|Acquired Immunodeficiency Syndrome
|
July 2007 | Phase 3 |
| NCT00082498 | National Institute of Allergy and Infectious Diseases (NIAID)|AIDS Clinical Trials Group |
HIV Infections
|
May 2004 | Phase 2 |
| NCT00243568 | Merck Sharp & Dohme LLC |
HIV Infections|Acquired Immunodeficiency Syndrome
|
September 1, 2005 | Phase 3 |
| NCT03631407 | Merck Sharp & Dohme LLC |
Colorectal Neoplasms
|
September 24, 2018 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 50 mg/mL ( 76.96 mM ; Need ultrasonic)
H 2 O : 25 mg/mL ( 38.48 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.5392 mL | 7.6959 mL | 15.3917 mL |
| 5 mM | 0.3078 mL | 1.5392 mL | 3.0783 mL |
| 10 mM | 0.1539 mL | 0.7696 mL | 1.5392 mL |
References
- [1] Tagat JR, et al. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonist. J Med Chem. 2004 May 6;47(10):2405-8.
- [2] Strizki JM, et al. Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2005 Dec;49(12):4911-9.
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