Isturisa (Osilodrostat)

  Cat. No.:  DC9974   Featured
Chemical Structure
928134-65-0
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
Osilodrostat is an inhibitor of aldosterone synthase and aromatase, for treating Cushing’s disease.
Cas No.: 928134-65-0
Chemical Name: (R)-4-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl)-3-fluorobenzonitrile
Synonyms: LCI699; LCI 699; LCI-699; Osilodrostat; Osilodrostat free base
SMILES: C1=C(C#N)C=C(F)C([C@@]([H])2CCC3=CN=CN23)=C1.P(O)(=O)(O)O
Formula: C13H10FN3
M.Wt: 227.237
Purity: >98%
Sotrage: 4°C for 1 year, -20°C for more than 2 years
Description: Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively.
Target: IC50: 2.5 nM (human 11β-hydroxylase), 0.7 nM (aldosterone synthase)[1]
In Vitro: Osilodrostat and pasireotide monotherapies are associated with significant changes in the histology and mean weights of the pituitary and adrenal glands, liver, and ovary/oviduct. Osilodrostat alone is associated with adrenocortical hypertrophy and hepatocellular hypertrophy. In combination, osilodrostat/pasireotide does not exacerbate any target organ changes and ameliorated the liver and adrenal gland changes observed with monotherapy. Cmax and AUC0–24h of osilodrostat and pasireotide increase in an approximately dose-proportional manner[1]. Osilodrostat treatment reduces urinary free cortisol in patients with Cushing's disease; 78.9% has normal urinary free cortisol at week 22. Treatment with osilodrostat is generally well tolerated[2].
Animal Administration: Rats: Sixty male and 60 female rats are randomized into single-sex groups to receive daily doses of pasireotide (0.3 mg/kg/day, subcutaneously), osilodrostat (20 mg/kg/day, orally), osilodrostat/pasireotide in combination (low dose, 1.5/0.03 mg/kg/day; mid-dose, 5/0.1 mg/kg/day; or high dose, 20/0.3 mg/kg/day), or vehicle for 13 weeks[1].
References: [1]. Li L, et al. Osilodrostat (LCI699), a potent 11β-hydroxylase inhibitor, administered in combination with the multireceptor-targeted somatostatin analog pasireotide: A 13-week study in rats. Toxicol Appl Pharmacol. 2015 Aug 1;286(3):224-33. [2]. Fleseriu M, et al. Osilodrostat, a potent oral 11β-hydroxylase inhibitor: 22-week, prospective, Phase II study in Cushing's disease. Pituitary. 2016 Apr;19(2):138-48.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC70000 Lysyllysyllysine Lysyllysyllysine is a cationic moietie that may be used in the construction of gene delivery vectors and DNA nanoparticles.
DC33580 DODMA DODMA, also known as MBN 305A is a a cationic lipid containing the unsaturated long-chain (18:1) oleic acid inserted at both the sn-1 and sn-2 positions. It has been used in the composition of lipospomes formulated as stable nucleic acid lipid particles that can encapsulate siRNA or other small molecules to be used for drug delivery
DC33636 DOTAP DOTAP, also known as 1,2-Dioleoyl-3-trimethylammoniumpropane, is a cationic liposome-forming compound used for transfection of DNA, RNA, and other negatively charged molecules into eukaryotic cells. It has been used in gene delivery vectors for gene ther
DC46471 RP101988 RP101988, the major active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC50s of 0.19 nM and 32.8 nM for S1PR1 and S1PR5, respectivlely.
DC45184 Hydrofurimazine Hydrofurimazine is a NanoLuc substrate whose enhanced aqueous solubility allows delivery of higher doses to mice. Hydrofurimazine enables sensitive bioluminescence imaging for either prolonged light production of high sensitivity.
DC37901 PD-173212 PD-173212 is a small molecule N-type calcium channel blocker.
DC37333 N,N-Diethyl-p-toluamide N,N-Diethyl-p-toluamide is a mosquito repellent.
DC37321 AI3-15902 AI3-15902 is a biochemical.
DC37283 Methyl phenylcarbamate Methyl phenylcarbamate is a biochemical.
DC37252 Ampyrone Ampyrone is a metabolite of AMINOPYRINE with analgesic and anti-inflammatory properties. It is used as a reagent for biochemical reactions producing peroxides or phenols. Ampyrone stimulates LIVER MICROSOMES and is also used to measure extracellular water.
X