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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
MK-3207 HCl (MK-3207; MK3207), the hydrochloride salt of MK3207, is a novel, potent and orally bioactive CGRP (Calcitonin gene related peptide) receptor antagonist with important biological activity. It exhibits CGRP at IC50 and Ki of 0.12 nM and 0.022 nM, respectively.
Targets |
CGRP receptor ( IC50 = 0.12 nM )
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
MK-3207 and 40 pM rat amylin are combined in amylin binding assays, and then 25 μg of CTR/RAMP1 or 25 μg of CTR/RAMP3 membranes are added. The mixture is then incubated for three hours at room temperature in binding buffer (10 mM HEPES, 5 mM MgCl2, and 0.2% bovine serum albumin) in a volume of one milliliter. As the radioligand in calcitonin binding assays, 25 μg of CTR membranes are used with 30 pM 125I-human calcitonin. Filtration through GF/B 96-well filter plates blocked with 0.5% polyethylenimine ends the incubation process. Prism is utilized for data analysis, and the equation Ki=IC50/1 + ([ligand]/KD is used to calculate the Ki value. Saturation binding experiments are used to calculate the KD value for each receptor.
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Animal Protocol |
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References |
Molecular Formula |
C31H29F2N5O3.HCL
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Molecular Weight |
594.05
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Exact Mass |
593.2
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CAS # |
957116-20-0
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Appearance |
Powder
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SMILES |
C1CCC2(C1)C(=O)N([C@@H](CN2)C3=CC(=CC(=C3)F)F)CC(=O)NC4=CC5=C(C[C@@]6(C5)C7=C(NC6=O)N=CC=C7)C=C4.Cl
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InChi Key |
VWKNXYACOMQRBX-KZCKSIIFSA-N
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InChi Code |
InChI=1S/C31H29F2N5O3.ClH/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);1H/t25-,30+;/m0./s1
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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;hydrochloride
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6834 mL | 8.4168 mL | 16.8336 mL | |
5 mM | 0.3367 mL | 1.6834 mL | 3.3667 mL | |
10 mM | 0.1683 mL | 0.8417 mL | 1.6834 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Selected CGRP Receptor Antagonists.ACS Med Chem Lett.2010 Jan 12;1(1):24-9. th> |
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Model predictedvs. observed blood flow by MK-3207 plasma concentration at two capsaicin doses (300 and 1000 μg).Br J Clin Pharmacol.2015 May;79(5):831-7. td> |
Simulated mean response of inhibition (%) of capsaicin-induced dermal vasodilatation (CIDV) byMK-3207vs.plasma concentrations ofMK-3207.Br J Clin Pharmacol.2015 May;79(5):831-7. td> |