THIQ

CAS No. 312637-48-2

THIQ( —— )

Catalog No. M21961 CAS No. 312637-48-2

THIQ is a selective melanocortin-4 receptor (MC4R)?agonist (hMC4R and rMC4R with IC50 of 1.2 nM and 0.6 nM , respectively).?

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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5MG 88 In Stock
10MG 170 In Stock
25MG 354 In Stock
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Biological Information

  • Product Name
    THIQ
  • Note
    Research use only, not for human use.
  • Brief Description
    THIQ is a selective melanocortin-4 receptor (MC4R)?agonist (hMC4R and rMC4R with IC50 of 1.2 nM and 0.6 nM , respectively).?
  • Description
    THIQ is a selective melanocortin-4 receptor (MC4R)?agonist (hMC4R and rMC4R with IC50 of 1.2 nM and 0.6 nM , respectively).?THIQ,?a small molecule agonist of the MC4R, on the cell surface expression and signaling of ten intracellularly retained MC4R mutants using different cell lines.?THIQ increased the cell surface expression of three mutants (N62S, C84R, and C271Y) and two of them (N62S and C84R) had increased signaling in HEK293 cells.THIQ increased the signaling of two other mutants (P78L and P260Q) without increasing their cell surface expression in HEK293 cells.?In neuronal cells, THIQ exhibited a more potent effect, correcting the cell surface expression and signaling of seven mutants (N62S, I69R, P78L, C84R, W174C, P260Q, and C271Y).
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    Melanocortin Receptor
  • Recptor
    melanocortin-4 receptor (MC4R)
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    312637-48-2
  • Formula Weight
    589.17
  • Molecular Formula
    C33H41ClN6O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:245 mg/ml(415.84 mM; Need ultrasonic)
  • SMILES
    Clc1ccc(C[C@@H](NC(=O)[C@H]2Cc3ccccc3CN2)C(=O)N2CCC(Cn3cncn3)(CC2)C2CCCCC2)cc1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Huang H, et al. A small molecule agonist THIQ as a novel pharmacoperone for intracellularly retainedmelanocortin-4 receptor mutants. Int J Biol Sci. 2014 Jul 20;10(8):817-24.2. Sun X , Liu M , Gao L , et al. A novel tetrahydroisoquinoline (THIQ) analogue induces mitochondria-dependent apoptosis[J]. European Journal of Medicinal Chemistry, 2018:S0223523418302526.3. Sebhat IK, et al. 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-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist. J Med Chem. 2002 Oct 10;45(21):4589-93.
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