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MedKoo Cat#: 535181 | Name: Asundexian
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Asundexian, also known as BAY2433334 and BI1265162, is a blood coagulation factor XIa inhibitor. Asundexian binds directly to the active site of FXIa and thereby inhibits its activity. Asundexian inhibits human FXIa in buffer with an IC50 of 1 nM. BAY 2433334 is a promising development candidate for once-daily oral anticoagulation; it is being evaluated in phase 2 dose-finding studies in patients at risk of thrombosis.

Chemical Structure

Asundexian
Asundexian
CAS#2064121-65-7

Theoretical Analysis

MedKoo Cat#: 535181

Name: Asundexian

CAS#: 2064121-65-7

Chemical Formula: C26H21ClF4N6O4

Exact Mass: 592.1249

Molecular Weight: 592.94

Elemental Analysis: C, 52.67; H, 3.57; Cl, 5.98; F, 12.82; N, 14.17; O, 10.79

Price and Availability

Size Price Availability Quantity
5mg USD 850.00 2 Weeks
10mg USD 1,550.00 2 Weeks
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Synonym
Asundexian; BI1265162; BI-1265162; BI 1265162; BAY2433334; BAY 2433334; BAY-2433334;
IUPAC/Chemical Name
(S)-4-(2-(4-(5-chloro-2-(4-(trifluoromethyl)-1H-1,2,3-triazol-1-yl)phenyl)-5-methoxy-2-oxopyridin-1(2H)-yl)butanamido)-2-fluorobenzamide
InChi Key
XYWIPYBIIRTJMM-IBGZPJMESA-N
InChi Code
InChI=1S/C26H21ClF4N6O4/c1-3-19(25(40)33-14-5-6-15(24(32)39)18(28)9-14)36-11-21(41-2)17(10-23(36)38)16-8-13(27)4-7-20(16)37-12-22(34-35-37)26(29,30)31/h4-12,19H,3H2,1-2H3,(H2,32,39)(H,33,40)/t19-/m0/s1
SMILES Code
O=C(NC1=CC(F)=C(C(N)=O)C=C1)[C@H](CC)N(C=C2OC)C(C=C2C3=CC(Cl)=CC=C3N4C=C(C(F)(F)F)N=N4)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 592.94 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Piccini JP, Caso V, Connolly SJ, Fox KAA, Oldgren J, Jones WS, Gorog DA, Durdil V, Viethen T, Neumann C, Mundl H, Patel MR; PACIFIC-AF Investigators. Safety of the oral factor XIa inhibitor asundexian compared with apixaban in patients with atrial fibrillation (PACIFIC-AF): a multicentre, randomised, double-blind, double-dummy, dose-finding phase 2 study. Lancet. 2022 Apr 9;399(10333):1383-1390. doi: 10.1016/S0140-6736(22)00456-1. Epub 2022 Apr 3. PMID: 35385695. 2: Heitmeier S, Visser M, Tersteegen A, Dietze-Torres J, Glunz J, Gerdes C, Laux V, Stampfuss J, Roehrig S. Pharmacological profile of asundexian, a novel, orally bioavailable inhibitor of factor XIa. J Thromb Haemost. 2022 Jun;20(6):1400-1411. doi: 10.1111/jth.15700. Epub 2022 Mar 25. Erratum in: J Thromb Haemost. 2022 Oct;20(10):2448. PMID: 35289054; PMCID: PMC9313898. 3: Rao SV, Kirsch B, Bhatt DL, Budaj A, Coppolecchia R, Eikelboom J, James SK, Jones WS, Merkely B, Keller L, Hermanides RS, Campo G, Ferreiro JL, Shibasaki T, Mundl H, Alexander JH; PACIFIC AMI Investigators. A Multicenter, Phase 2, Randomized, Placebo-Controlled, Double-Blind, Parallel-Group, Dose-Finding Trial of the Oral Factor XIa Inhibitor Asundexian to Prevent Adverse Cardiovascular Outcomes After Acute Myocardial Infarction. Circulation. 2022 Oct 18;146(16):1196-1206. doi: 10.1161/CIRCULATIONAHA.122.061612. Epub 2022 Aug 27. Erratum in: Circulation. 2022 Dec 6;146(23):e330. PMID: 36030390. 4: Shoamanesh A, Mundl H, Smith EE, Masjuan J, Milanov I, Hirano T, Agafina A, Campbell B, Caso V, Mas JL, Dong Q, Turcani P, Christensen H, Ferro JM, Veltkamp R, Mikulik R, De Marchis GM, Robinson T, Lemmens R, Stepien A, Greisenegger S, Roine R, Csiba L, Khatri P, Coutinho J, Lindgren AG, Demchuk AM, Colorado P, Kirsch B, Neumann C, Heenan L, Xu L, Connolly SJ, Hart RG; PACIFIC-Stroke Investigators. Factor XIa inhibition with asundexian after acute non- cardioembolic ischaemic stroke (PACIFIC-Stroke): an international, randomised, double-blind, placebo-controlled, phase 2b trial. Lancet. 2022 Sep 24;400(10357):997-1007. doi: 10.1016/S0140-6736(22)01588-4. Epub 2022 Sep 2. PMID: 36063821. 5: Galli M, Laborante R, Ortega-Paz L, Franchi F, Rollini F, D'Amario D, Capodanno D, Tremoli E, Gibson CM, Mehran R, Angiolillo DJ. Factor XI Inhibitors in Early Clinical Trials: A Meta-analysis. Thromb Haemost. 2023 Jun;123(6):576-584. doi: 10.1055/a-2043-0346. Epub 2023 Feb 25. PMID: 36841245. 6: Gómez-Outes A, Suárez-Gea ML, Pérez-Cabeza AI, García-Pinilla JM. Pharmacotherapy for stroke prevention in nonvalvular atrial fibrillation: current strategies and future directions. Expert Opin Pharmacother. 2022 Dec;23(17):1941-1955. doi: 10.1080/14656566.2022.2149323. Epub 2022 Nov 27. PMID: 36398362. 7: Greco A, Laudani C, Spagnolo M, Agnello F, Faro DC, Finocchiaro S, Legnazzi M, Mauro MS, Mazzone PM, Occhipinti G, Rochira C, Scalia L, Capodanno D. Pharmacology and Clinical Development of Factor XI Inhibitors. Circulation. 2023 Mar 14;147(11):897-913. doi: 10.1161/CIRCULATIONAHA.122.062353. Epub 2023 Mar 13. PMID: 36913497. 8: Fiebig L, Helmes S, Kaiser M, Werner D. Determination of asundexian and its metabolite M-10 in human plasma by LC-MS/MS. Bioanalysis. 2023 Feb;15(4):197-206. doi: 10.4155/bio-2022-0107. Epub 2023 Apr 11. PMID: 37040422. 9: Mailer RK, Renné T. Commentary on "Pharmacological profile of asundexian, a novel, orally bioavailable inhibitor of factor XIa": Small molecule factor XIa inhibitor asundexian allows for safer anticoagulation. J Thromb Haemost. 2022 Jun;20(6):1309-1311. doi: 10.1111/jth.15722. PMID: 35596514. 10: Gailani D. Making anticoagulation safer. Lancet. 2022 Apr 9;399(10333):1360-1361. doi: 10.1016/S0140-6736(22)00563-3. Epub 2022 Apr 3. PMID: 35385696; PMCID: PMC9540354. 11: Kanefendt F, Brase C, Unger S, Kubitza D. Effects of Tablet Formulation, Food, or Gastric pH on the Bioavailability of Asundexian. Clin Pharmacol Drug Dev. 2023 Feb;12(2):219-230. doi: 10.1002/cpdd.1207. Epub 2022 Dec 11. PMID: 36507617; PMCID: PMC10107294. 12: Correction to: A Multicenter, Phase 2, Randomized, Placebo-Controlled, Double-Blind, Parallel-Group, Dose-Finding Trial of the Oral Factor XIa Inhibitor Asundexian to Prevent Adverse Cardiovascular Outcomes After Acute Myocardial Infarction. Circulation. 2022 Dec 6;146(23):e330. doi: 10.1161/CIR.0000000000001115. Epub 2022 Dec 5. Erratum for: Circulation. 2022 Oct 18;146(16):1196-1206. PMID: 36469599. 13: Fredenburgh JC, Weitz JI. News at XI: moving beyond factor Xa inhibitors. J Thromb Haemost. 2023 Jul;21(7):1692-1702. doi: 10.1016/j.jtha.2023.04.021. Epub 2023 Apr 26. PMID: 37116752.