THIQ

SKU: orb1298894

Description

THIQ is a potent and selective agonist of the melanocortin-4 receptor (MC4R), demonstrating high affinity with IC50 values of 1.2 nM for human and 0.6 nM for rat receptors. This small molecule is a valuable research tool for studying energy homeostasis and obesity in both in vitro binding assays and in vivo metabolic studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 312637-48-2
• MW: 589.17
• Purity: 99.74% (May vary between batches)
• Formula: C₃₃H₄₁ClN₆O₂
• SMILES: ClC1=CC=C(C[C@@H](NC(=O)[C@H]2CC3=CC=CC=C3CN2)C(=O)N2CCC(CN3C=NC=N3)(CC2)C2CCCCC2)C=C1
• Target: Melanocortin Receptor
• Solubility: DMSO:245 mg/mL (415.84 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (8.49 mM)

Bioactivity

• Target IC50:
  MC4R (rat):0.6 nM|MC4R (human):1.2 nM
• In Vitro:
  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).

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

affinity, activity, Inhibitor, MC Receptor, melanocortin, Melanocortin Receptor, melanocortin-4 receptor (MC4R), MelanocortinReceptor, erectile, eliciting, mutant, inhibit, selective, THIQ

Compound Identifiers

PubChem CID

9938402