THIQ CAS: 312637-48-2
MF: C33H41ClN6O2
MW: 589.17
A selective melanocortin 4 receptor agonist.

THIQ (CAS 312637-48-2)

THIQ | CAS 312637-48-2 is rated 5.0 out of 5 by 1.
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Alternate Names: N-[(1R)-1-[(4-Chlorophenyl)methyl]-2-[4-cyclohexyl-4-(1H-1,2,4-trazol-1-ylmethyl)-1-piperidinyl]-2-oxoethyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide
Application: THIQ is a selective melanocortin 4 receptor agonist
CAS Number: 312637-48-2
Purity: >95%
Molecular Weight: 589.17
Molecular Formula: C33H41ClN6O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

THIQ is a selective and potent melanocortin 4 receptor (MC4-R) agonist (IC50 values are 1.2, 761 and 2067 nM for human MC4-R, MC3-R and MC1-R respectively). Following systemic administration, enhances intracavernosal pressure and stimulates erectile activity in rats ex copula.


References

Sebhat et al (2002) Design and pharmacology of N-[(3R)-1,2,3,4-Tetrahydroisoquinolinium-3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-methyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective melanocortin subtype-4 receptor agonist. J.Med.Chem. 45 4589. Martin et al (2002) Activation of melanocortin MC4 receptors increases erectile activity in rats ex copula. Eur.J.Pharmacol. 454 71. Mutulis et al (2004) New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of "THIQ". J.Med.Chem. 47 4613.

Physical State :
Solid
Solubility :
Soluble in water (10 mM).
Storage :
Store at -20° C
Density :
1.34 g/cm3 (Predicted)
Refractive Index :
n20D 1.68 (Predicted)
IC50 :
MC4-R: IC50 = 1.2 nM; MC3-R: IC50 = 761 nM; Melanocortin receptor 5: IC50 = 1.58 µM (rat); MC1-R: IC50 = 2.07 µM
Ki Data :
MC4-R: Ki= 3 nM (human); MC3-R: Ki= 125 nM (human); MC1-R: Ki= 300 nM (human); MC5-R: Ki= 860 nM (human)
pK Values :
pKa: 13.82 (Predicted), pKb: 7.86 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
RTECS :
NW6986600
PubChem CID :
9938402
MDL Number :
MFCD09970598
SMILES :
Clc1ccc(cc1)C[[email protected]@H](NC(=O)[[email protected]@H]1NCc2ccccc2C1)C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Molden et al Molden et al. (Pubmed ID 26418335) found that the MC4R agonist, THIQ, activated prolonged cAMP signaling even after its withdrawal. -SCBT Publication Review
Date published: 2015-05-17
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