MK-3207

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

MedKoo CAT#: 525647

CAS#: 957118-49-9 (free base)

Description: MK-3207 is a potent and orally active calcitonin gene-related peptide receptor antagonist. Calcitonin gene related peptide (CGRP) receptor antagonists are effective acute migraine treatments. (Ki = 0.024 nM).

Chemical Structure

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MK-3207
CAS# 957118-49-9 (free base)
Instruction

Theoretical Analysis

MedKoo Cat#: 525647
Name: MK-3207
CAS#: 957118-49-9 (free base)
Chemical Formula: C31H29F2N5O3
Exact Mass: 557.22
Molecular Weight: 557.602
Elemental Analysis: C, 66.78; H, 5.24; F, 6.81; N, 12.56; O, 8.61

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 957116-20-0 (HCl)   957118-49-9 (free base)    

Synonym: MK-3207; MK3207; MK 3207

IUPAC/Chemical Name: 2-[(8R)-8-(3,5-difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(2R)-2'-oxospiro[1,3-dihydroindene-2,3'-1H-pyrrolo[2,3-b]pyridine]-5-yl]acetamide

InChi Key: AZAANWYREOQRFB-SETSBSEESA-N

InChi Code: InChI=1S/C31H29F2N5O3/c32-21-10-19(11-22(33)13-21)25-16-35-31(7-1-2-8-31)29(41)38(25)17-26(39)36-23-6-5-18-14-30(15-20(18)12-23)24-4-3-9-34-27(24)37-28(30)40/h3-6,9-13,25,35H,1-2,7-8,14-17H2,(H,36,39)(H,34,37,40)/t25-,30+/m0/s1

SMILES Code: O=C(NC1=CC2=C(C[C@]3(C4=CC=CN=C4NC3=O)C2)C=C1)CN(C5=O)[C@H](C6=CC(F)=CC(F)=C6)CNC75CCCC7

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:

Preparing Stock Solutions

The following data is based on the product molecular weight 557.60 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Li CC, Vermeersch S, Denney WS, Kennedy WP, Palcza J, Gipson A, Han TH, Blanchard R, De Lepeleire I, Depré M, Murphy MG, Van Dyck K, de Hoon JN. Characterizing the PK/PD relationship for inhibition of capsaicin-induced dermal vasodilatation by MK-3207, an oral calcitonin gene related peptide receptor antagonist. Br J Clin Pharmacol. 2015 May;79(5):831-7. doi: 10.1111/bcp.12547. PubMed PMID: 25377933; PubMed Central PMCID: PMC4415719.
2: Hewitt DJ, Aurora SK, Dodick DW, Goadsby PJ, Ge YJ, Bachman R, Taraborelli D, Fan X, Assaid C, Lines C, Ho TW. Randomized controlled trial of the CGRP receptor antagonist MK-3207 in the acute treatment of migraine. Cephalalgia. 2011 Apr;31(6):712-22. doi: 10.1177/0333102411398399. Epub 2011 Mar 7. PubMed PMID: 21383045.
3: Bell IM, Gallicchio SN, Wood MR, Quigley AG, Stump CA, Zartman CB, Fay JF, Li CC, Lynch JJ, Moore EL, Mosser SD, Prueksaritanont T, Regan CP, Roller S, Salvatore CA, Kane SA, Vacca JP, Selnick HG. Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist. ACS Med Chem Lett. 2010 Jan 12;1(1):24-9. doi: 10.1021/ml900016y. eCollection 2010 Apr 8. PubMed PMID: 24900170; PubMed Central PMCID: PMC4007836.
4: Salvatore CA, Moore EL, Calamari A, Cook JJ, Michener MS, O'Malley S, Miller PJ, Sur C, Williams DL Jr, Zeng Z, Danziger A, Lynch JJ, Regan CP, Fay JF, Tang YS, Li CC, Pudvah NT, White RB, Bell IM, Gallicchio SN, Graham SL, Selnick HG, Vacca JP, Kane SA. Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist. J Pharmacol Exp Ther. 2010 Apr;333(1):152-60. doi: 10.1124/jpet.109.163816. Epub 2010 Jan 11. PubMed PMID: 20065019.