CI 992 - CAS 135704-06-2
Catalog number: 135704-06-2
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C33H52N6O7S2
Molecular Weight:
708.94
COA:
Inquire
Targets:
Renin
Description:
CI 992 is a renin inhibitor originated by Pfizer. Preclinical trials for Hypertension in USA was discontinued in 1994.
Purity:
98%
Appearance:
Powder
Synonyms:
CI 992; CI992; CI-992. N-(4-morpholinylsulfonyl)-L-phenylalanyl-3-(2-amino-4-thiazolyl)-N-[(1S,2R,3S)-1-(cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl]-L-alaninamide; [1S-(1R*,2S*,3R*)]- N-(4-morpholinylsulfonyl)-L-phenylalanyl-3-(2-amino-4-thiazolyl)-N-[1-(cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl]-L-alaninamide; PD 134672; PD134672; PD-134672;
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Hypertension
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
IYMYORIPWWCOOB-VFFRCKCKSA-N
InChI:
1S/C33H52N6O7S2/c1-22(2)17-29(40)30(41)26(18-23-9-5-3-6-10-23)36-27(20-25-21-47-33(34)35-25)31(42)37-32(43)28(19-24-11-7-4-8-12-24)38-48(44,45)39-13-15-46-16-14-39/h4,7-8,11-12,21-23,26-30,36,38,40-41H,3,5-6,9-10,13-20H2,1-2H3,(H2,34,35)(H,37,42,43)/t26-,
Canonical SMILES:
C([C@@H](N[C@H]([C@H]([C@H](CC(C)C)O)O)CC1CCCCC1)Cc1nc(sc1)N)(=O)NC([C@@H](NS(=O)(=O)N1CCOCC1)Cc1ccccc1)=O
Current Developer:
Originator Pfizer
1.Pharmacokinetics and pharmacodynamics of CI-992 following intravenous and oral administration to cynomolgus monkeys.
Cook JA;Burger PJ;Michniewicz BM;Nordblom GD;Hicks GW;Kaplan C;Ryan MJ Biopharm Drug Dispos. 1998 Apr;19(3):185-91.
The purpose of this study was to characterize CI-992 pharmacokinetics and pharmacokinetics/pharmacodynamics (PK/PD) in sodium deplete monkeys. Panels of monkeys were administered CI-992 as a 1 h intravenous infusions (0.1 and 1 mg kg-1) or as single oral doses (0, 10, 50, and 100 mg kg-1). Mean arterial blood pressure (MABP) was monitored and serial blood samples were collected up to 24 h postdose. Plasma CI-992 concentrations were quantitated by radioimmunoassay. Pharmacokinetic parameters were calculated by noncompartmental methods. PK/PD relationships were assessed by standard methods. Oral bioavailability of CI-992 in the monkeys was < 2%; steady-state volume of distribution was 0.67 L kg-1; clearance was 10.4 mL min-1 kg-1. Following oral administration, tmax generally occurred 6-9 h postadministration; plasma CI-992 concentrations increased with increasing dose between 10 and 50 mg kg-1, but did not change appreciably from 50 to 100 mg kg-1. After intravenous administration, change in MABP was correlated with plasma CI-992 concentration through an effect compartment model in which the maximum achievable effect was a 22 mm Hg decrease in MABP; the steady-state concentration which produced half the maximum effect was 11 ng mL-1.
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