MedKoo Cat#: 414745 | Name: Paltusotine HCl

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 HCl
Paltusotine HCl
CAS#2172875-40-8 (2HCl)

Theoretical Analysis

MedKoo Cat#: 414745

Name: Paltusotine HCl

CAS#: 2172875-40-8 (2HCl)

Chemical Formula: C27H24Cl2F2N4O

Exact Mass:

Molecular Weight: 529.41

Elemental Analysis: C, 61.26; H, 4.57; Cl, 13.39; F, 7.18; N, 10.58; O, 3.02

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
2361216-83-1 (HCl); 2172870-89-0 (free base) 2172875-40-8 (2HCl)
Synonym
Paltusotine hydrochloride; Paltusotine HCl; Paltusotine; CRN00808; CRN-00808; CRN 00808;
IUPAC/Chemical Name
Benzonitrile, 3-(4-(4-amino-1-piperidinyl)-3-(3,5-difluorophenyl)-6-quinolinyl)-2-hydroxy-, hydrochloride (1:2)
InChi Key
GVTGYFQUBMBIAE-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H22F2N4O.2ClH/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;2*1H
SMILES Code
N#CC1=CC=CC(C2=CC=C3N=CC(C4=CC(F)=CC(F)=C4)=C(N5CCC(N)CC5)C3=C2)=C1O.[H]Cl.[H]Cl
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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 529.41 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.