A CGRP receptor antagonist (Ki = 0.77 μM); binds selectively to the human CGRP receptor complex over the adrenomedullin receptor complexes in HEK293 cells (Kis = >100 and 29 μM for CRLR with RAMP2 and 3

MK-0974 – 1 mg

Brand:
Cayman
CAS:
781649-09-0
Storage:
-20
UN-No:
Non-Hazardous - /

MK-0974 is an orally bioavailable antagonist of the calcitonin gene-related peptide (CGRP) receptor complex (Ki = 0.77 μM), which is composed of the calcitonin receptor-like receptor (CRLR) and receptor activity modifying protein 1 (RAMP1).{38703} MK-0974 binds selectively to the human CGRP receptor complex, over the adrenomedullin receptor complexes, which are composed of CRLR and RAMP2 or RAMP3 (Kis = >100 and 29 μM, respectively, in HEK293 cells). MK-0974 also binds to rhesus, canine, and rat CGRP receptor complexes (Kis = 1.2, 1,204, and 1,192 nM, respectively). MK-0974 inhibits cAMP accumulation stimulated by CGRP (Item No. 24405) with an IC50 value of 2.2 nM in HEK293 cells expressing the CGRP receptor complex. Ex vivo, MK-0974 (5 μM) reduces CGRP-induced vasodilation in isolated human meningeal arteries.{38704} MK-0974 also inhibits vasodilation induced by topical application of capsaicin (Item No. 92350) in rhesus monkeys (EC50 = 127 nM).{38703}  

 

Available on backorder

Add to quotes
SKU: 23960 - 1 mg Category:

Description

A CGRP receptor antagonist (Ki = 0.77 μM); binds selectively to the human CGRP receptor complex over the adrenomedullin receptor complexes in HEK293 cells (Kis = >100 and 29 μM for CRLR with RAMP2 and 3, respectively); inhibits CGRP-induced cAMP accumulation in HEK293 cells expressing the CGRP receptor complex (IC50 = 2.2 nM); reduces CGRP-induced vasodilation in isolated human meningeal arteries; inhibits vasodilation induced by topical application of capsaicin in rhesus monkeys (EC50 = 127 nM)

Formal name: N-[(3R,6S)-6-(2,3-difluorophenyl)hexahydro-2-oxo-1-(2,2,2-trifluoroethyl)-1H-azepin-3-yl]-4-(2,3-dihydro-2-oxo-1H-imidazo[4,5-b]pyridin-1-yl)-1-piperidinecarboxamide

Synonyms: 

Molecular weight: 566.5

CAS: 781649-09-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Research Area|Cardiovascular System|Vasculature|Vasoconstriction

Related products

  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 5 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 5 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 10 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 50 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page