AT-1459 - CAS 294658-50-7
Catalog number: 294658-50-7
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C29H42N6O4
Molecular Weight:
538.32
COA:
Inquire
Targets:
Others
Description:
AT-1459 is a novel, direct thrombin inhibitor with antithrombotic efficacy (Ki = 4.9 nM).
Purity:
≥95%
Appearance:
Solid powder
Synonyms:
AT-1459; AT 1459; AT1459; UNII-JWP323ABVS; Butanoic acid, 4-​[[(3S)​-​1-​[2-​[(2S)​-​2-​[2-​[6-​(aminoiminomethyl)​-​1-​ethyl-​1H-​indol-​2-​yl]​ethyl]​-​1-​pyrrolidinyl]​-​2-​oxoethyl]​hexahydro-​2-​oxo-​1H-​azepin-​3-​yl]​amino]​-
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
Thrombin Inhibitor
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
Quantity:
Milligrams-Grams
InChIKey:
DTJAQQZJSTVZRK-UPVQGACJSA-N
InChI:
1S/C29H42N6O4/c1-2-34-23(17-20-10-11-21(28(30)31)18-25(20)34)13-12-22-7-6-16-35(22)26(36)19-33-15-4-3-8-24(29(33)39)32-14-5-9-27(37)38/h10-11,17-18,22,24,32H,2-9,12-16,19H2,1H3,(H3,30,31)(H,37,38)/t22-,24-/m0/s1
Canonical SMILES:
CCn1c(cc2c1cc(cc2)C(=N)N)CC[C@@H]3CCCN3C(=O)CN4CCCC[C@@H](C4=O)NCCCC(=O)O
1.The antithrombotic efficacy of AT-1459, a novel, direct thrombin inhibitor, in rat models of venous and arterial thrombosis.
Cho JH;Yun CH;Seo HS;Koga T;Dan T;Koo BA;Kim HY Thromb Haemost. 2001 Dec;86(6):1512-20.
The antithrombotic efficacy of AT-1459, a novel, direct thrombin inhibitor (Ki = 4.9 nM) was evaluated in rat models of venous thrombosis combined with a bleeding time test and arterial thrombosis. After drugs were given by i. v. bolus injection plus a continuous infusion, the ID50, (a dose that exhibits 50% inhibition of thrombus formation over each vehicle group) values of AT-1459, argatroban, and dalteparin were 0.04 mg/kg plus 0.04 mg/kg/h, 0.1 mg/kg plus 0.4 mg/ kg/h, and 13.0 IU/kg plus 26.0 IU/kg/h, respectively, in the venous thrombosis study. The BT2 (a dose that causes 2-fold prolongation of bleeding time over each vehicle group) values of AT-1459, argatroban, and dalteparin were 0.9 mg/kg plus 0.9 mg/kg/h, 1.0 mg/kg plus 0.6 mg/kg/h, and 345.5 IU/kg plus 691.0 IU/kg/h in the rat tail transection model. The ratios of BT2/ID50 of AT-1459, argatroban, and dalteparin were 22.5, 10.0, and 26.6, respectively. In a rat model of arterial thrombosis induced by topical FeCl2 application, intravenous administration of AT-1459, argatroban, and dalteparin improved the vessel patency significantly (P < 0.01) at 0.6 mg/kg plus 0.6 mg/kg/h, 0.6 mg/kg plus 2.4 mg/kg/h, and 300 IU/kg plus 600 IU/kg/h, respectively.
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