WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H522499
CAS#: 1159500-34-1
Description: Selatogrel, also known as ACT-246475, is a reversible, selective, and potent antagonist of the platelet P2Y12 receptor. It therefore acts as a platelet aggregation inhibitor. Selatogrel dose-dependently blocks thrombus formation and displays a wide therapeutic window.
Hodoodo Cat#: H522499
Name: Selatogrel
CAS#: 1159500-34-1
Chemical Formula: C28H39N6O8P
Exact Mass: 618.26
Molecular Weight: 618.630
Elemental Analysis: C, 54.36; H, 6.35; N, 13.59; O, 20.69; P, 5.01
This product is not in stock, which may be available by custom synthesis.
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Synonym: ACT-246475; ACT 246475; ACT246475; Selatogrel.
IUPAC/Chemical Name: ((R)-3-(4-(butoxycarbonyl)piperazin-1-yl)-2-(6-((S)-3-methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carboxamido)-3-oxopropyl)phosphonic acid
InChi Key: FYXHWMQPCJOJCH-GMAHTHKFSA-N
InChi Code: InChI=1S/C28H39N6O8P/c1-3-4-16-42-28(37)33-14-12-32(13-15-33)27(36)23(19-43(38,39)40)30-26(35)22-17-24(34-11-10-21(18-34)41-2)31-25(29-22)20-8-6-5-7-9-20/h5-9,17,21,23H,3-4,10-16,18-19H2,1-2H3,(H,30,35)(H2,38,39,40)/t21-,23-/m0/s1
SMILES Code: O=C(N1CCN(C([C@@H](NC(C2=NC(C3=CC=CC=C3)=NC(N4CC[C@@H](C4)OC)=C2)=O)CP(O)(O)=O)=O)CC1)OCCCC
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, not in water
Shelf Life: >2 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:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 618.63 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.
| 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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Milluzzo RP, Franchina GA, Capodanno D, Angiolillo DJ. Selatogrel, a novel P2Y12 inhibitor: a review of the pharmacology and clinical development. Expert Opin Investig Drugs. 2020 Jun;29(6):537-546. doi: 10.1080/13543784.2020.1764533. Epub 2020 May 12. PMID: 32396484.
2: Silvain J, Zeitouni M, Kerneis M. Selatogrel for Acute Myocardial Infarction: The Promise and Challenges of Self-Medication. J Am Coll Cardiol. 2020 May 26;75(20):2598-2601. doi: 10.1016/j.jacc.2020.03.054. PMID: 32439009.
3: Sinnaeve P, Fahrni G, Schelfaut D, Spirito A, Mueller C, Frenoux JM, Hmissi A, Bernaud C, Ufer M, Moccetti T, Atar S, Valgimigli M. Subcutaneous Selatogrel Inhibits Platelet Aggregation in Patients With Acute Myocardial Infarction. J Am Coll Cardiol. 2020 May 26;75(20):2588-2597. doi: 10.1016/j.jacc.2020.03.059. PMID: 32439008.
4: Parker WAE, Storey RF. Pharmacology and potential role of selatogrel, a subcutaneous platelet P2Y12 receptor antagonist. Expert Opin Emerg Drugs. 2020 Mar;25(1):1-6. doi: 10.1080/14728214.2020.1729121. Epub 2020 Feb 17. PMID: 32064955.
5: Baumann M, Lack B, Guillaumat I, Murphy MJ, Riederer MA. The potency of selatogrel, a reversible antagonist of the P2Y12 receptor, is affected by calcium concentration. Platelets. 2021 Jan 11:1-10. doi: 10.1080/09537104.2020.1869711. Epub ahead of print. PMID: 33427002.
6: Schilling U, Dingemanse J, Voors-Pette C, Romeijn C, Dogterom P, Ufer M. Effect of Rifampin-Mediated OATP1B1 and OATP1B3 Transporter Inhibition on the Pharmacokinetics of the P2Y12 Receptor Antagonist Selatogrel. Clin Transl Sci. 2020 Sep;13(5):886-890. doi: 10.1111/cts.12774. Epub 2020 Mar 31. PMID: 32166864; PMCID: PMC7485944.
7: Storey RF, Gurbel PA, Ten Berg J, Bernaud C, Dangas GD, Frenoux JM, Gorog DA, Hmissi A, Kunadian V, James SK, Tanguay JF, Tran H, Trenk D, Ufer M, Van der Harst P, Van't Hof AWJ, Angiolillo DJ. Pharmacodynamics, pharmacokinetics, and safety of single-dose subcutaneous administration of selatogrel, a novel P2Y12 receptor antagonist, in patients with chronic coronary syndromes. Eur Heart J. 2020 Sep 1;41(33):3132-3140. doi: 10.1093/eurheartj/ehz807. PMID: 31994703; PMCID: PMC7556746.
8: Ufer M, Huynh C, van Lier JJ, Caroff E, Fischer H, Dingemanse J. Absorption, distribution, metabolism and excretion of the P2Y12 receptor antagonist selatogrel after subcutaneous administration in healthy subjects. Xenobiotica. 2020 Apr;50(4):427-434. doi: 10.1080/00498254.2019.1646440. Epub 2019 Aug 7. PMID: 31322041.
9: Schilling U, Dingemanse J, Dobrow M, Baumann M, Riederer MA, Juif PE, Ufer M. Insights from In Vitro and Clinical Data to Guide Transition from the Novel P2Y12 Antagonist Selatogrel to Clopidogrel, Prasugrel, and Ticagrelor. Thromb Haemost. 2021 Jun;121(6):755-766. doi: 10.1055/s-0040-1721773. Epub 2021 Jan 7. PMID: 33412611.
10: Beavers CJ, Effoe SA, Dobesh PP. Selatogrel: A Novel Subcutaneous P2Y12 Inhibitor. J Cardiovasc Pharmacol. 2021 Jun 8. doi: 10.1097/FJC.0000000000001079. Epub ahead of print. PMID: 34132688.
11: Crescence L, Darbousset R, Caroff E, Hubler F, Riederer MA, Panicot-Dubois L, Dubois C. Selatogrel, a reversible P2Y12 receptor antagonist, has reduced off-target interference with haemostatic factors in a mouse thrombosis model. Thromb Res. 2021 Apr;200:133-140. doi: 10.1016/j.thromres.2021.01.026. Epub 2021 Feb 6. PMID: 33610885.
12: Henrich A, Claussen CH, Dingemanse J, Krause A. Pharmacokinetic/pharmacodynamic modeling of drug interactions at the P2Y12 receptor between selatogrel and oral P2Y12 antagonists. CPT Pharmacometrics Syst Pharmacol. 2021 Jul;10(7):735-747. doi: 10.1002/psp4.12641. Epub 2021 May 30. PMID: 33955698; PMCID: PMC8302241.
13: Hulot JS, Montalescot G. Do we need a new P2Y12 receptor antagonist? Eur Heart J. 2020 Sep 1;41(33):3141-3143. doi: 10.1093/eurheartj/ehz862. PMID: 31845967.
14: Schilling U, Dingemanse J, Ufer M. Pharmacokinetics and Pharmacodynamics of Approved and Investigational P2Y12 Receptor Antagonists. Clin Pharmacokinet. 2020 May;59(5):545-566. doi: 10.1007/s40262-020-00864-4. PMID: 32056160.
15: Parker WAE, Storey RF. Novel approaches to P2Y12 inhibition and aspirin dosing. Platelets. 2021 Jan 2;32(1):7-14. doi: 10.1080/09537104.2020.1714574. Epub 2020 Jan 19. PMID: 31957518.
16: Rout A, Sukhi A, Chaudhary R, Bliden KP, Tantry US, Gurbel PA. Investigational drugs in phase II clinical trials for acute coronary syndromes. Expert Opin Investig Drugs. 2020 Jan;29(1):33-47. doi: 10.1080/13543784.2020.1708324. Epub 2020 Jan 3. PMID: 31869253.
17: Juif PE, Boehler M, Dobrow M, Ufer M, Dingemanse J. Clinical Pharmacology of the Reversible and Potent P2Y12 Receptor Antagonist ACT-246475 After Single Subcutaneous Administration in Healthy Male Subjects. J Clin Pharmacol. 2019 Jan;59(1):123-130. doi: 10.1002/jcph.1296. Epub 2018 Aug 8. PMID: 30088663.
18: Baldoni D, Bruderer S, Krause A, Gutierrez M, Gueret P, Astruc B, Dingemanse J. A new reversible and potent P2Y12 receptor antagonist (ACT-246475): tolerability, pharmacokinetics, and pharmacodynamics in a first-in-man trial. Clin Drug Investig. 2014 Nov;34(11):807-18. doi: 10.1007/s40261-014-0236-8. PMID: 25331625.
