Camlipixant
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MedKoo CAT#: 121067

CAS#: 1621164-74-6

Description: Camlipixant, also known as BLU-5937, is a potent, selective and non-competitive P2X3 homotrimeric receptor antagonist. The IC50 of BLU-5937 for hP2X3 homotrimeric and hP2X2/3 heterotrimeric receptors was established at 25 nM and >24 μM, respectively. Furthermore, BLU-5937 (500 nM) was able to block αβ-meATP-induced sensitization and firing activity of isolated primary nociceptors in rat dorsal root ganglions (DRGs), through P2X3 homotrimeric receptor antagonism. In a guinea pig cough model, BLU-5937 (0.3, 3 and 30 mg/kg, oral) significantly reduced, in a dose-dependent fashion, the histamine-induced enhancement in the number of citric acid-induced coughs. BLU-5937 (3 and 30 mg/kg, oral) was also shown to reduce significantly and dose-dependently the ATP-induced enhancement of citric acid-induced coughs in the guinea pig.

Chemical Structure

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Camlipixant
CAS# 1621164-74-6
Instruction

Theoretical Analysis

MedKoo Cat#: 121067
Name: Camlipixant
CAS#: 1621164-74-6
Chemical Formula: C23H24F2N4O4
Exact Mass: 458.18
Molecular Weight: 458.466
Elemental Analysis: C, 60.26; H, 5.28; F, 8.29; N, 12.22; O, 13.96

Price and Availability

Size Price Availability Quantity
10mg USD 350 2 Weeks
25mg USD 550 2 Weeks
50mg USD 950 2 Weeks
100mg USD 1650 2 Weeks
200mg USD 2650 2 Weeks
1g USD 6950 2 Weeks
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Synonym: Camlipixant; BLU-5937; BLU 5937; BLU5937;

IUPAC/Chemical Name: methyl (2S)-2-({2-[2,6-difluoro-4-(methylcarbamoyl)phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl}methyl)morpholine-4-carboxylate

InChi Key: SEHLMRJSQFAPCJ-HNNXBMFYSA-N

InChi Code: InChI=1S/C23H24F2N4O4/c1-13-4-5-29-18(11-15-12-28(6-7-33-15)23(31)32-3)21(27-19(29)8-13)20-16(24)9-14(10-17(20)25)22(30)26-2/h4-5,8-10,15H,6-7,11-12H2,1-3H3,(H,26,30)/t15-/m0/s1

SMILES Code: CC1=CC(N2C=C1)=NC(C3=C(F)C=C(C(NC)=O)C=C3F)=C2C[C@H]4CN(C(OC)=O)CCO4

Appearance: To be determined

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: P2X3 receptors are ATP ion-gated channels located on primary afferent neurons. ATP released from damaged or inflamed tissues in the airways acts on P2X3 receptors of primary afferent neurons, triggering depolarization and action potentials that are transmitted centrally and interpreted as urge to cough. There are strong preclinical and clinical evidence supporting the role of P2X3 receptors in hypersensitization of the cough reflex, leading to chronic cough. By inhibiting P2X3 receptors on the primary sensory neurons, BLU-5937 would inhibit the hypersensitization of the cough reflex and, hence, the exaggerated cough experienced in chronic cough patients. BLU-5937 is being developed for the treatment of unexplained, refractory chronic cough. BLU-5937 exhibits excellent drug-like characteristics, including good oral bioavailability, low predicted clearance in human, no blood-brain barrier permeability and high safety margin versus human predicted efficacious exposure. BLU-5937 is currently in clinical phase I development stage.

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 458.47 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Burgoyne DS. Managed care considerations for the treatment of chronic cough. Am J Manag Care. 2022 Sep;28(9 Suppl):S166-S174. doi: 10.37765/ajmc.2022.89245. PMID: 36198075.


2: Dicpinigaitis PV, McGarvey LP, Canning BJ. P2X3-Receptor Antagonists as Potential Antitussives: Summary of Current Clinical Trials in Chronic Cough. Lung. 2020 Aug;198(4):609-616. doi: 10.1007/s00408-020-00377-8. Epub 2020 Jul 13. PMID: 32661659.


3: Marucci G, Dal Ben D, Buccioni M, Martí Navia A, Spinaci A, Volpini R, Lambertucci C. Update on novel purinergic P2X3 and P2X2/3 receptor antagonists and their potential therapeutic applications. Expert Opin Ther Pat. 2019 Dec;29(12):943-963. doi: 10.1080/13543776.2019.1693542. Epub 2019 Nov 20. PMID: 31726893.


4: Garceau D, Chauret N. BLU-5937: A selective P2X3 antagonist with potent anti- tussive effect and no taste alteration. Pulm Pharmacol Ther. 2019 Jun;56:56-62. doi: 10.1016/j.pupt.2019.03.007. Epub 2019 Mar 20. PMID: 30902655.