| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Osilodrostat phosphate (formerly LCI-699; LCI699; Isturisa), the phosphate salt of Osilodrostat, is a potent 11β-hydroxylase inhibitor that has been approved in 2020 for the treatment of Cushing's disease.
| ln Vitro |
Cortisol and aldosterone are inhibited by osilodrostat (LCI699; 0.01-10 µM; HAC15 cells, 17 primary human adrenocortical cell cultures, and pituitary adenoma cells). Osilodrostat has a minor impact on adrenal androgens and inhibits the build-up of corticosterone and 11-deoxycortisol [2].
|
|---|---|
| ln Vivo |
In Ang-II and ACTH-stimulated Sprague Dawley rats, osilodrostat (LCI699; 0.1-100 mg/kg; oral; once) phosphate reduces the production of aldosterone and corticosterone [1]. In dTG rats, oral osilodrostat phosphate (LCI699; 3-100 mg/kg; daily for 52 weeks) lowers mean arterial pressure and increases survival [1].
|
| Animal Protocol |
Animal/Disease Models: dTG rat[1]
Doses: 3, 10, 30 and 100 mg/kg Route of Administration: Oral; one time/day for 52 weeks Experimental Results: Shortened LV fractional shortening (systolic and diastolic), LV Isovolumic relaxation time to RR (IVRT/RR) ratio and cardiomyocyte size were normalized and diminished LV mass in a dose-dependent manner. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No information is available on the use of osilodrostat during breastfeeding. Because of the potential for serious adverse reactions, such as adrenal insufficiency, in the breastfed infant, breastfeeding is not recommended during treatment with osilodrostat and should be avoided until 1 week after the final dose. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
|
| Additional Infomation |
See also: Osilodrostat (has active moiety).
Drug Indication Isturisa is indicated for the treatment of endogenous Cushing's syndrome in adults. |
| Molecular Formula |
C13H13FN3O4P
|
|---|---|
| Molecular Weight |
325.2321870327
|
| Exact Mass |
325.062
|
| CAS # |
1315449-72-9
|
| Related CAS # |
Osilodrostat;928134-65-0
|
| PubChem CID |
71009737
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
22
|
| Complexity |
387
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C1CC2=CN=CN2[C@H]1C3=C(C=C(C=C3)C#N)F.OP(=O)(O)O
|
| InChi Key |
FMCPYRDGUZBOJZ-BTQNPOSSSA-N
|
| InChi Code |
InChI=1S/C13H10FN3.H3O4P/c14-12-5-9(6-15)1-3-11(12)13-4-2-10-7-16-8-17(10)13;1-5(2,3)4/h1,3,5,7-8,13H,2,4H2;(H3,1,2,3,4)/t13-;/m1./s1
|
| Chemical Name |
4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile;phosphoric acid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ≥ 200 mg/mL (~614.95 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0747 mL | 15.3737 mL | 30.7475 mL | |
| 5 mM | 0.6149 mL | 3.0747 mL | 6.1495 mL | |
| 10 mM | 0.3075 mL | 1.5374 mL | 3.0747 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
