MedKoo Cat#: 585098 | Name: Paltusotine free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Paltusotine, also known as CRN00808, is a somatostatin receptor agonist. Paltusotine showed no direct inhibition of major cytochrome P450 enzymes or the hERG ion channel and had sufficient exposure in rats and excellent exposure in dogs upon oral dosing. In pharmacodynamic studies, Paltusotine dose-dependently suppressed growth hormone (GH) secretion induced by an exogenous growth-hormone-releasing hormone (GHRH) challenge in both male and female rats following a single oral dose and suppressed IGF-1 levels with repeated oral administration in both rats and dogs.

Chemical Structure

Paltusotine free base
Paltusotine free base
CAS#2172870-89-0 (free base)

Theoretical Analysis

MedKoo Cat#: 585098

Name: Paltusotine free base

CAS#: 2172870-89-0 (free base)

Chemical Formula: C27H22F2N4O

Exact Mass: 456.1762

Molecular Weight: 456.50

Elemental Analysis: C, 71.04; H, 4.86; F, 8.32; N, 12.27; O, 3.50

Price and Availability

Size Price Availability Quantity
5mg USD 950.00 2 Weeks
10mg USD 1,650.00 2 Weeks
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Related CAS #
2361216-83-1 (HCl); 2172870-89-0 (free base) 2172875-40-8 (2HCl)
Synonym
Paltusotine; CRN00808; CRN-00808; CRN 00808;
IUPAC/Chemical Name
3-[4-(4-aminopiperidin-1-yl)-3-(3,5- difluorophenyl)quinolin-6-yl]-2-hydroxybenzonitrile
InChi Key
GHILNKWBALQPDP-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H22F2N4O/c28-19-10-18(11-20(29)13-19)24-15-32-25-5-4-16(22-3-1-2-17(14-30)27(22)34)12-23(25)26(24)33-8-6-21(31)7-9-33/h1-5,10-13,15,21,34H,6-9,31H2
SMILES Code
N#CC1=CC=CC(C2=CC=C3N=CC(C4=CC(F)=CC(F)=C4)=C(N5CCC(N)CC5)C3=C2)=C1O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 456.50 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z. Prospect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine. Nat Commun. 2023 Feb 21;14(1):962. doi: 10.1038/s41467-023-36673-z. PMID: 36810324; PMCID: PMC9944328. 2: Zhao J, Wang S, Markison S, Kim SH, Han S, Chen M, Kusnetzow AK, Rico- Bautista E, Johns M, Luo R, Struthers RS, Madan A, Zhu Y, Betz SF. Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist. ACS Med Chem Lett. 2022 Dec 10;14(1):66-74. doi: 10.1021/acsmedchemlett.2c00431. PMID: 36655128; PMCID: PMC9841592. 3: McLaren DS, Murray RD. Paltusotine, a novel oral somatostatin receptor ligand in the management of acromegaly. J Clin Endocrinol Metab. 2022 Dec 30:dgac762. doi: 10.1210/clinem/dgac762. Epub ahead of print. PMID: 36582134. 4: Gadelha MR, Gordon MB, Doknic M, Mezősi E, Tóth M, Randeva H, Marmon T, Jochelson T, Luo R, Monahan M, Madan A, Ferrara-Cook C, Struthers RS, Krasner A. ACROBAT Edge: Safety and efficacy of switching injected SRLs to oral paltusotine in patients with acromegaly. J Clin Endocrinol Metab. 2022 Nov 10:dgac643. doi: 10.1210/clinem/dgac643. Epub ahead of print. PMID: 36353760. 5: Madan A, Markison S, Betz SF, Krasner A, Luo R, Jochelson T, Lickliter J, Struthers RS. Paltusotine, a novel oral once-daily nonpeptide SST2 receptor agonist, suppresses GH and IGF-1 in healthy volunteers. Pituitary. 2022 Apr;25(2):328-339. doi: 10.1007/s11102-021-01201-z. Epub 2022 Jan 9. PMID: 35000098; PMCID: PMC8894159. 6: Gadelha MR, Wildemberg LE, Kasuki L. The Future of Somatostatin Receptor Ligands in Acromegaly. J Clin Endocrinol Metab. 2022 Jan 18;107(2):297-308. doi: 10.1210/clinem/dgab726. PMID: 34618894; PMCID: PMC8764337. 7: Antunes X, Kasuki L, Gadelha MR. New and emerging pharmacological treatment options for acromegaly. Expert Opin Pharmacother. 2021 Aug;22(12):1615-1623. doi: 10.1080/14656566.2021.1908998. Epub 2021 Apr 8. PMID: 33783289.