1802425-99-5
1802425-99-5
Chemical Structure
Milvexian
Synonym(s): BMS-986177; JNJ-70033093
- CAS No.: 1802425-99-5
- Formula:C28H23Cl2F2N9O2
- Molecular Weight:626.44
IUPAC Name: (5R,9S)-9-(4-(5-chloro-2-(4-chloro-1H-1,2,3-triazol-1-yl)phenyl)-6-oxopyrimidin-1(6H)-yl)-21-(difluoromethyl)-5-methyl-21H-3-aza-1(4,2)-pyridina-2(5,4)-pyrazolacyclononaphan-4-one
InChIKey: FSWFYCYPTDLKON-CMJOXMDJSA-N
SMILES: O=C(NC1=C2N(C(F)F)N=C1)[C@H](C)CCC[C@H](N(C=NC(C3=CC(Cl)=CC=C3N4N=NC(Cl)=C4)=C5)C5=O)C6=CC2=CC=N6
Biological Activity: Milvexian is an orally bioavailable, small-molecule, reversible, direct antagonists of factor Xia, with the Ki of 0.11, 0.38, 0.64, 490, 350 nM for human, rabbit, dog, rat, mouse, respectively. Milvexian shows anti-thrombosis activity in vitro and in vivo, and can be used for thrombus study[1].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Milvexian | 99.93% | Milvexian is an orally bioavailable, small-molecule, reversible, direct antagonists of factor Xia, with the Ki of 0.11, 0.38, 0.64, 490, 350 nM for human, rabbit, dog, rat, mouse, respectively. Milvexian shows anti-thrombosis activity in vitro and in vivo, and can be used for thrombus study. | ||||||||||||||||||||
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Milvexian TFA | Milvexian TFA (BMS-986177 TFA) is a factor XIa inhibitor with biological activity to prevent venous thromboembolism. Milvexian TFA was effective in reducing the occurrence of venous thromboembolism in patients undergoing knee replacement surgery. Milvexian TFA has good selectivity and shows significant inhibitory effects on plasma kallikrein and trypsin. Milvexian TFA has a bioavailability of 32%, which means it has a high absorption rate in the body. Milvexian TFA showed a relatively low risk of bleeding in clinical trials. | |||||||||||||||||||||
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Asundexian | 99.80% | Asundexian (BAY 2433334) is an orally active coagulation factor Xia (FXIa) inhibitor. Asundexian binds directly, potently, and reversibly to the active site of FXIa and thereby inhibits its activity. Asundexian inhibits human FXIa in buffer with an IC50 of 1 nM. | ||||||||||||||||||||
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(R)-Asundexian | 99.97% | (R)-Asundexian ((R)-BAY-2433334) is the enantiomer of Asundexian (HY-137431). (R)-Asundexian can be used in studies of cardiovascular disease, edema, and ophthalmic disease. | ||||||||||||||||||||
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FXIa-IN-9 | FXIa-IN-9 (compound 3f) is a potent and selective FXIa inhibitor. FXIa-IN-9 can bind with FXIa and form hydrogen bond (human FXIa Ki: 0.17 nM, rabbit FXIa Ki: 0.5 nM). FXIa-IN-9 also has anticoagulant activity, and can be used in the research of thromboembolic diseases such as atrial fibrillation, stroke, myocardial infarction, deep vein thrombosis, and pulmonary embolism. | |||||||||||||||||||||
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FXIa-IN-10 | FXIa-IN-10 (Compound 3f) is a potent activated factor XI (FXIa) inhibitor with an Ki of 0.17 nM. FXIa-IN-10 has good oral bioavailability. | |||||||||||||||||||||
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BET bromodomain inhibitor 4 | 99.66% | BET bromodomain inhibitor 4 (example 7) is an inhibitor of the BET bromodomain domain. | ||||||||||||||||||||
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TYM-3-98 | 99.56% | TYM-3-98 is a selective inhibitor for PI3Kδ, with an IC50 of 7.1 nM. TYM-3-98 inhibits proliferationso of B-lymphoma cells. TYM-3-98 inhibits PI3K/AKT/mTOR signaling pathway through induction of apoptosis. TYM-3-98 exhibits good pahrmacokinetic characters and antitumor efficacy in mouse/rat model, without significant toxicity. | ||||||||||||||||||||
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FXIa-IN-15 | FXIa-IN-15 (Compound (S)-10h) is an inhibitor for Factor XIa (FXIa) and plasma kallikrein (PKa) with an IC50 of 0.38 nM and 59.2 nM. FXIa-IN-15 exhibits anticoagulant efficacy, that extends 50% activated partial thromboplastin time (aPTT) with EC1.5X of 0.55 μM. | |||||||||||||||||||||
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FXIa-IN-16 | FXIa-IN-16 is an orally active selective FXIa inhibitor with an IC50 of 0.19 nM. FXIa-IN-16 exerts highly selective competitive inhibition on endogenous FXIa, blocks the thrombin amplification loop to inhibit thrombosis, while preserving exogenous physiological hemostatic function. FXIa-IN-16 can be used in thrombosis-related research. | |||||||||||||||||||||
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ONO-7684 | ONO-7684 (ONO-5450598) is an orally active coagulation factor XIa (FXIa) inhibitor with a Ki value of 2 nM against human FXIa. ONO-7684 inhibits human FXIa in a competitive and reversible manner, reduces factor XI coagulation activity, prolongs activated partial thromboplastin time in a dose-dependent manner, and exerts no significant effects on PT/INR and the activity of related serine proteases. ONO-7684 exerts antithrombotic effects in vivo without prolonging bleeding time. ONO-7684 can be used in studies related to thromboembolic diseases. | |||||||||||||||||||||
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