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Cat. No. Product Name CAS No. Information
PC-70112

ATR-101

133825-81-7

ATR-101 (PD-132301, Nevanimibe) is a selective and potent inhibitor of ACAT1 with IC50 of 52 nM; induces H295R cell apoptosis, causes mitochondrial hyperpolarization, reactive oxygen release, and ATP depletion, caspase-3/7 activation, and membrane permeabilization; decreases the formation of cholesteryl esters and increases FC levels in H295R adrenocortical carcinoma cells; inhibits the establishment and impeds the growth of ACC-derived H295R cell xenografts in mice; orally active.

Cushing Disease

Phase 2 Clinical

PC-35460

ATR-101 free base

133825-80-6 ATR-101 (PD-132301, Nevanimibe) is a selective and potent inhibitor of ACAT1 with IC50 of 52 nM; induces H295R cell apoptosis, causes mitochondrial hyperpolarization, reactive oxygen release, and ATP depletion, caspase-3/7 activation, and membrane permeabilization; decreases the formation of cholesteryl esters and increases FC levels in H295R adrenocortical carcinoma cells; inhibits the establishment and impeds the growth of ACC-derived H295R cell xenografts in mice; orally active.

Cushing Disease

Phase 2 Clinical

PC-61987

AZD 4017

1024033-43-9 AZD4017 is a potent, selective, and orally bioavailable human 11β-HSD1 with IC50 of 7 nM, shows no significant activity against 11β-HSD1 and 17β-HSD1, 17β-HSD3 (IC50>30 uM); AZD4017 is inactive (<25% inhibition at 10 μM) against Cytochrome P450 enzymes (CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4), and lower potency against the mouse, rat and dog 11β-HSD1 (IC50=750-4000 nM); demonstrates the dose dependent inhibition of 11β-HSD1 in vivo.

Cushing Disease

Phase 2 Clinical

PC-61498

Relacorilant

1496510-51-0 A potent, selective glucocorticoid receptor (GR) antagonist with Ki of 7.2 nM in the HepG2 TAT assay; displays high selectivity over the progesterone receptor, androgen receptor, and estrogen receptor and no affinity for the other receptors; has excellent potency, selectivity, and oral bioavailability in several species with acceptable physicochemical properties.

Cushing Disease

Phase 2 Clinical

PC-46000

Pasireotide L-aspartate salt

396091-77-3 A potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (pKi=8.2/9.0/9.1/<7.0/9.9 for sst1/2/3/4/5, respectively); effectively inhibits GHRH-induced growth hormone release in primary cultures of rat pituitary cells with IC50 of 0.4 nM, also potently suppresses GH secretion in rats.

Cushing's Disease

Approved

PC-45999

Pasireotide ditrifluoroacetate

A potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (pKi=8.2/9.0/9.1/<7.0/9.9 for sst1/2/3/4/5, respectively); effectively inhibits GHRH-induced growth hormone release in primary cultures of rat pituitary cells with IC50 of 0.4 nM, also potently suppresses GH secretion in rats.

Cushing's Disease

Approved

PC-44950

Pasireotide

396091-73-9 A potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (pKi=8.2/9.0/9.1/<7.0/9.9 for sst1/2/3/4/5, respectively); effectively inhibits GHRH-induced growth hormone release in primary cultures of rat pituitary cells with IC50 of 0.4 nM, also potently suppresses GH secretion in rats.

Cushing's Disease

Approved

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