| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 25 nM (hP2X3), >24000 nM (hP2X2/3), 92 nM (rP2X3), 1820 nM (rP2X2/3), 126 nM (gpP2X3), 3450 nM (gpP2X2/3)[1]
Camlipixant selectively targets the P2X3 homotrimeric receptor, a ligand-gated ion channel involved in cough reflex signaling. It exhibits potent antagonism with an IC50 of 25 nM against the human P2X3 receptor. Camlipixant displays 1500-fold selectivity for human P2X3 over human P2X2/3 heterotrimers, with an IC50 of 92 nM for rat P2X3. Its non-competitive mechanism of action contributes to its improved safety profile regarding taste alteration. |
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| ln Vitro |
BLU-5937, or camlipixant, at 500 nM, inhibits ATP-mediated DRG neuron sensitization [1].
In vitro, camlipixant inhibits P2X3 homotrimeric receptor-mediated currents in HEK293 cells expressing human P2X3, with an IC50 of 25 nM. It shows 1500-fold selectivity over human P2X2/3 heterotrimers. Camlipixant (500 nM) effectively inhibits P2X3-mediated sensitization of rat dorsal root ganglion (DRG) neurons, blocking ATP-mediated neuronal sensitization by inhibiting P2X3 homotrimeric receptors. The compound is non-competitive and orally active. |
| ln Vivo |
In guinea pigs, the histamine- and ATP-induced allergic cough is lessened by camlipixant (BLU-5937; 3–30 mg/kg; oral)[1]. When compared to control animals, camlipixant (BLU-5937; 10–20 mg/kg; ip) does not change taste perception[1]. Excellent drug-like characteristics of camlipixant (BLU-5937) include outstanding oral bioavailability, low expected human clearance, no penetration of the blood-brain barrier, and a great safety profile[1].
In vivo, camlipixant (0.3-30 mg/kg, orally) reduces histamine- and ATP-induced cough hypersensitivity in guinea pigs. It significantly reduces ATP- and histamine-induced enhancement in the number of citric acid-induced coughs. The compound does not alter taste perception in animal models, addressing a key limitation of other P2X3 antagonists such as gefapixant. Camlipixant is also being evaluated for its effects on P2X3-mediated pain signaling. |
| Enzyme Assay |
For in vitro receptor binding assays, HEK293 cells stably expressing human P2X3 receptors are pre-incubated with camlipixant at concentrations ranging from 0.1-1000 nM for 5-10 minutes. ATP (1-100 uM) is then applied to activate the receptor, and calcium influx is measured using a fluorescent calcium indicator (e.g., Fluo-4). IC50 values are calculated by fitting dose-response curves. For selectivity assays, similar experiments are performed on cells expressing P2X2/3 heterotrimers.
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| Cell Assay |
For cell-based assays, rat DRG neurons are cultured and treated with camlipixant at concentrations from 1-1000 nM for 30-60 minutes. Neurons are then stimulated with ATP (10 uM) to activate P2X3 homotrimeric receptors. Sensitization is assessed by measuring calcium influx or whole-cell patch-clamp recordings of ATP-evoked currents. Supernatants can be collected to measure neuropeptide release (e.g., substance P, CGRP). Cell viability is assessed by MTT or LDH assays.
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| Animal Protocol |
Animal/Disease Models: Male Dunkin Hartley guinea pigs[1]
Doses: 0.3, 3, 30 mg/kg Route of Administration: PO, approximately 2 h prior to tussive agent exposure Experimental Results: Dramatically decreased the histamine-induced enhancement in the number of citric acid-induced coughs. decreased Dramatically and dose-dependently the ATP-induced enhancement of citric acid-induced coughs. For in vivo efficacy studies, camlipixant is typically formulated in a suitable oral vehicle (e.g., 0.5% methylcellulose or 10% DMSO in saline). Guinea pigs are administered camlipixant orally (0.3-30 mg/kg) 1-2 hours before cough challenge. Cough is induced by inhalation of citric acid aerosol (0.4 M) for 10 minutes. The number of coughs is counted over the challenge period. Histamine or ATP inhalation can also be used to induce cough hypersensitivity. Taste alteration is assessed using brief-access taste tests or two-bottle preference tests. |
| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for camlipixant are limited in publicly available sources. The compound is described as orally active and bioavailable, with properties suitable for once- or twice-daily oral dosing. In preclinical species, camlipixant demonstrates good plasma exposure and brain penetration. For specific PK parameters (Cmax, Tmax, t1/2, oral bioavailability), researchers should consult primary research articles or conduct pilot studies.
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| Toxicity/Toxicokinetics |
Published toxicology data for camlipixant are limited. In animal studies at doses up to 30 mg/kg (oral), no significant adverse effects have been reported. The compound's high selectivity for P2X3 homotrimers over P2X2/3 heterotrimers is believed to underlie its reduced taste alteration side effect profile. Comprehensive toxicology studies have been conducted to support clinical development. Researchers should consult published safety data for detailed information.
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| References | |
| Additional Infomation |
Camlipixant is being investigated in the clinical trial NCT05600777 (a 24-week study of the efficacy and safety of BLU-5937 in treating refractory chronic cough in adults (CALM-2)).
Selective P2X3 receptor antagonist Camlipixant is in clinical development for refractory chronic cough. It has been studied in Phase 2 clinical trials (e.g., NCT04088838, NCT04264468) and has shown efficacy in reducing cough frequency with a favorable safety profile and no significant taste disturbance. It represents a next-generation P2X3 antagonist with improved selectivity. Camlipixant is not yet approved for clinical use. The compound should be stored at -20degC, protected from light. |
| Molecular Formula |
C23H24F2N4O4
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|---|---|
| Molecular Weight |
458.457872390747
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| Exact Mass |
458.18
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| Elemental Analysis |
C, 60.26; H, 5.28; F, 8.29; N, 12.22; O, 13.96
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| CAS # |
1621164-74-6
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| PubChem CID |
76955630
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| Appearance |
White to off-white solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
704
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC1C=C(C(NC)=O)C=C(C=1C1=C(C[C@H]2CN(C(=O)OC)CCO2)N2C=CC(C)=CC2=N1)F
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| InChi Key |
SEHLMRJSQFAPCJ-HNNXBMFYSA-N
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| 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
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| Chemical Name |
methyl (2S)-2-[[2-[2,6-difluoro-4-(methylcarbamoyl)phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]morpholine-4-carboxylate
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| Synonyms |
Camlipixant; BLU-5937; BLU 5937; BLU5937;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (218.12 mM)
DMSO: 100 mg/mL (218.12 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1812 mL | 10.9061 mL | 21.8122 mL | |
| 5 mM | 0.4362 mL | 2.1812 mL | 4.3624 mL | |
| 10 mM | 0.2181 mL | 1.0906 mL | 2.1812 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.
Link: https://clinicaltrials.gov/ct2/show/NCT05600777
Conditions:Cough|Refractory Chronic CoughLink: https://clinicaltrials.gov/ct2/show/NCT07519395
Conditions:Irritable Bowel SyndromeLink: https://clinicaltrials.gov/ct2/show/NCT06222892
Conditions:Cough
Title:A 52-Week Study of the Efficacy and Safety of BLU-5937 in Adults With Refractory Chronic Cough
Status:Active, not recruiting
updateDate:2025-06-10
Ctid:NCT05599191
Link: https://clinicaltrials.gov/ct2/show/NCT05599191
Conditions:Cough|Refractory Chronic CoughLink: https://clinicaltrials.gov/ct2/show/NCT05959447
Conditions:Cough|HealthyLink: https://clinicaltrials.gov/ct2/show/NCT05899829
Conditions:Cough|HealthyLink: https://clinicaltrials.gov/ct2/show/NCT06179537
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT04693195
Conditions:Chronic Pruritus|Atopic DermatitisLink: https://clinicaltrials.gov/ct2/show/NCT04678206
Conditions:Refractory Chronic CoughLink: https://clinicaltrials.gov/ct2/show/NCT03979638
Conditions:Chronic Refractory CoughLink: https://clinicaltrials.gov/ct2/show/NCT03638180
Conditions:CoughProducts are for research use only; We do not sell to patients
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