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MedKoo Cat#: 596535 | Name: MK 0852

Description:

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

MK 0852 is a cyclic heptapeptide antagonist of the platelet GP IIb/IIIa.

Chemical Structure

MK 0852
MK 0852
CAS#138199-64-1

Theoretical Analysis

MedKoo Cat#: 596535

Name: MK 0852

CAS#: 138199-64-1

Chemical Formula: C34H47N9O12S3

Exact Mass: 869.2506

Molecular Weight: 869.98

Elemental Analysis: C, 46.94; H, 5.45; N, 14.49; O, 22.07; S, 11.06

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
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Synonym
MK 0852; MK-0852; MK0852; L-367,073; L 367,073; L367,073; L 367073; L-367073; L367073;
IUPAC/Chemical Name
(6S,9R,14R,17S,23S,25aR)-9-acetamido-6-(2-amino-2-oxoethyl)-23-(4-(aminomethyl)benzyl)-17-(carboxymethyl)-1,1-dimethyl-5,8,16,19,22,25-hexaoxoicosahydro-1H,3H-thiazolo[4,3-p][1,2]dithia[5,8,11,14,17,20]hexaazacyclotricosine-14-carboxylic acid
InChi Key
IHTQUFFCUYSOIH-SBTHHMAGSA-N
InChi Code
InChI=1S/C34H47N9O12S3/c1-16(44)38-22-13-57-58-14-23(33(54)55)42-29(50)20(10-26(47)48)39-25(46)12-37-28(49)19(8-17-4-6-18(11-35)7-5-17)40-31(52)27-34(2,3)56-15-43(27)32(53)21(9-24(36)45)41-30(22)51/h4-7,19-23,27H,8-15,35H2,1-3H3,(H2,36,45)(H,37,49)(H,38,44)(H,39,46)(H,40,52)(H,41,51)(H,42,50)(H,47,48)(H,54,55)/t19-,20-,21-,22-,23-,27+/m0/s1
SMILES Code
NCc1ccc(C[C@@H]2NC([C@@H]3C(C)(SCN3C([C@H](CC(N)=O)NC([C@H](CSSC[C@@H](C(O)=O)NC([C@@H](NC(CNC2=O)=O)CC(O)=O)=O)NC(C)=O)=O)=O)C)=O)cc1
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
>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

Preparing Stock Solutions

The following data is based on the product molecular weight 869.98 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: Zhao L, Bath P, Lösche W, Heptinstall S. Platelet-monocyte interaction and GPIIb/IIIa blockade. Thromb Haemost. 2004 Oct;92(4):888-90. PubMed PMID: 15467921. 2: Zhao L, Bath PM, May J, Lösche W, Heptinstall S. P-selectin, tissue factor and CD40 ligand expression on platelet-leucocyte conjugates in the presence of a GPIIb/IIIa antagonist. Platelets. 2003 Nov-Dec;14(7-8):473-80. Erratum in: Platelets. 2004 Feb;15(1):63. PubMed PMID: 14713516. 3: Zhao L, Bath PM, Fox S, May J, Judge H, Lösche W, Heptinstall S. The effects of GPIIb-IIIa antagonists and a combination of three other antiplatelet agents on platelet-leukocyte interactions. Curr Med Res Opin. 2003;19(3):178-86. PubMed PMID: 12803731. 4: Lages B, Weiss HJ. Greater inhibition of platelet procoagulant activity by antibody-derived glycoprotein IIb--IIIa inhibitors than by peptide and peptidomimetic inhibitors. Br J Haematol. 2001 Apr;113(1):65-71. PubMed PMID: 11328283. 5: Kingma JG Jr, Plante S, Bogaty P. Platelet GPIIb/IIIa receptor blockade reduces infarct size in a canine model of ischemia-reperfusion. J Am Coll Cardiol. 2000 Dec;36(7):2317-24. PubMed PMID: 11127479. 6: Greenberg HE, Wissel P, Barrett J, Barchowsky A, Gould R, Farrell D, Panebianco D, Hand E, Gillen L, Goldberg MR, Bjornsson TD. Antiplatelet effects of MK-852, a platelet fibrinogen receptor antagonist, in healthy volunteers. J Clin Pharmacol. 2000 May;40(5):496-507. PubMed PMID: 10806603. 7: Storey RF, Wilcox RG, Heptinstall S. Differential effects of glycoprotein IIb/IIIa antagonists on platelet microaggregate and macroaggregate formation and effect of anticoagulant on antagonist potency. Implications for assay methodology and comparison of different antagonists. Circulation. 1998 Oct 20;98(16):1616-21. PubMed PMID: 9778326. 8: Bednar RA, Gaul SL, Hamill TG, Egbertson MS, Shafer JA, Hartman GD, Gould RJ, Bednar B. Identification of low molecular weight GP IIb/IIIa antagonists that bind preferentially to activated platelets. J Pharmacol Exp Ther. 1998 Jun;285(3):1317-26. PubMed PMID: 9618439. 9: Wittig K, Rothe G, Schmitz G. Inhibition of fibrinogen binding and surface recruitment of GpIIb/IIIa as dose-dependent effects of the RGD-mimetic MK-852. Thromb Haemost. 1998 Mar;79(3):625-30. PubMed PMID: 9531053. 10: Rossi G. [Superaspirin in the platelet aggregation inhibitor therapy]. Recenti Prog Med. 1997 Dec;88(12):590-1. Italian. PubMed PMID: 9522603. 11: Dubost DC, Kaufman MJ, Zimmerman JA, Bogusky MJ, Coddington AB, Pitzenberger SM. Characterization of a solid state reaction product from a lyophilized formulation of a cyclic heptapeptide. A novel example of an excipient-induced oxidation. Pharm Res. 1996 Dec;13(12):1811-4. PubMed PMID: 8987076. 12: May JA, Heptinstall S, Spangenberg P. Changes in the composition of the platelet cytoskeleton in response to ADP: effects of MK-852 and ARL 66096. Blood Coagul Fibrinolysis. 1996 Mar;7(2):221-4. PubMed PMID: 8735824. 13: Hoylaerts MF, Thys C, Stassen JM, Vermylen J. Dose-responses to inducers and inhibitors of platelet aggregation analysed via a micro-method. Blood Coagul Fibrinolysis. 1996 Mar;7(2):187-90. PubMed PMID: 8735815. 14: Cook JJ, Sitko GR, Bednar B, Condra C, Mellott MJ, Feng DM, Nutt RF, Shafer JA, Gould RJ, Connolly TM. An antibody against the exosite of the cloned thrombin receptor inhibits experimental arterial thrombosis in the African green monkey. Circulation. 1995 Jun 15;91(12):2961-71. PubMed PMID: 7796507. 15: Vickers S, Duncan CA, Yuan AS, Vyas KP. Disposition of MK-852, a fibrinogen receptor antagonist, in rats and dogs. Drug Metab Dispos. 1994 Jul-Aug;22(4):631-6. PubMed PMID: 7956740. 16: Larsson A, Lindahl TL. Inhibition of fibrinogen binding to platelets by MK-852, a new GPIIb/IIIa antagonist. Ups J Med Sci. 1994;99(2):121-9. PubMed PMID: 7716823. 17: Ramjit DR, Lynch JJ Jr, Sitko GR, Mellott MJ, Holahan MA, Stabilito II, Stranieri MT, Zhang G, Lynch RJ, Manno PD, et al. Antithrombotic effects of MK-0852, a platelet fibrinogen receptor antagonist, in canine models of thrombosis. J Pharmacol Exp Ther. 1993 Sep;266(3):1501-11. PubMed PMID: 8371153. 18: Yuan AS, Hand EL, Hichens M, Olah TV, Barrish A, Fernandez-Metzler C, Gilbert JD. Determination of MK-852, a new fibrinogen receptor antagonist, in plasma and urine by radioimmunoassay. J Pharm Biomed Anal. 1993 Jun;11(6):427-34. PubMed PMID: 8399513.