Capsazepine - CAS 138977-28-3
Catalog number: 138977-28-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
TRP Channel
Capsazepine, a benzazepine derivative, has been found to be a sensory neurone excitotoxin that could be used against hyperalgesic responses. IC50: 562 nM (Rat TRPV1).
> 95%
White to Light Yellow Solid
DMSO: ≥ 50 mg/mL
-20ºC Freeze
Capsazepine has been found to be a sensory neurone excitotoxin that could be used against hyperalgesic responses.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Melting Point:
Canonical SMILES:
1.Protective role of cannabinoid CB1 receptors and vascular effects of chronic administration of FAAH inhibitor URB597 in DOCA-salt hypertensive rats.
Baranowska-Kuczko M1, Kozłowska H2, Kloza M2, Karpińska O2, Toczek M2, Harasim E3, Kasacka I4, Malinowska B2. Life Sci. 2016 Mar 9. pii: S0024-3205(16)30164-3. doi: 10.1016/j.lfs.2016.03.014. [Epub ahead of print]
AIMS: This study examined whether the fall in blood pressure (BP) induced by the chronic inhibition of fatty acid amide hydrolase (FAAH) by URB597 in deoxycorticosterone acetate (DOCA-salt) hypertensive rats correlates with endocannabinoid-mediated vascular changes.
2.Involvement of TRPV1 in the Olfactory Bulb in Rimonabant-Induced Olfactory Discrimination Deficit.
Hu SS1. Chin J Physiol. 2016 Feb 29;59(1):21-32. doi: 10.4077/CJP.2016.BAE366.
Rimonabant is well recognized as a cannabinoid CB₁ receptor antagonist/inverse agonist. Rimonabant not only antagonizes the effects induced by exogenous cannabinoids and endocannabinoids at CB₁ receptors, it also exerts several pharmacological and behavioral effects independent of CB₁ receptor inactivation. For example, rimonabant can function as a low-potency mixed agonist/antagonist of the transient receptor potential vanilloid receptor 1 (TRPV1). Hence, it is important to explain the underlying mechanisms of the diverse physiological effects induced by rimonabant with caution. Interestingly, CB₁ receptor has recently been suggested to play a role in olfactory functions. Olfaction not only is involved in food intake, visual perception and social interaction, but also is proposed as a putative marker for schizophrenia and autism. Therefore, the present study aimed to investigate whether CB₁ receptor and TRPV1 played a role in olfactory functions.
3.The Transient Receptor Potential Vanilloid 1 (TRPV1) Antagonist Capsazepine Improves the Impaired Lung Mechanics during Endotoxemia.
Cabral LD1,2, Giusti-Paiva A1,2. Basic Clin Pharmacol Toxicol. 2016 Apr 19. doi: 10.1111/bcpt.12605. [Epub ahead of print]
Acute lung injury (ALI) caused by systemic inflammatory response remains a leading cause of morbidity and mortality in critically ill patients. Management of patients with sepsis is largely limited to supportive therapies, reflecting an incomplete understanding of the underlying pathophysiology. Furthermore, there have been limited advances in the treatments for ALI. In the present study, lung function and a histological analysis were performed to evaluate the impact of transient receptor potential vanilloid-1 receptor (TRPV1) antagonist (capsazepine; CPZ) on the lipopolysaccharide (LPS)-induced lung injury in mice. For this, adult mice pre-treated with CPZ or vehicle received intraperitoneal injections of LPS or saline and 24 hr after, the mice were anaesthetized, and lung mechanics was evaluated. The LPS-challenged mice exhibited substantial mechanical impairment, characterized by increases in respiratory system resistance, respiratory system elastance, tissue damping and tissue elastance.
4.Inflammatory stimuli acutely modulate peripheral taste function.
Kumarhia D1, He L1, McCluskey LP2. J Neurophysiol. 2016 Mar 23:jn.01104.2015. doi: 10.1152/jn.01104.2015. [Epub ahead of print]
Inflammation-mediated changes in taste perception can affect health outcomes in patients, but little is known about underlying mechanisms. In the current work, we hypothesized that proinflammatory cytokines directly modulate Na+transport in taste buds. To test this, we measured acute changes in Na+flux in polarized fungiform taste buds loaded with a Na+indicator dye. IL-1β elicited an amiloride-sensitive increase in Na+transport in taste buds. In contrast, TNF-α dramatically and reversibly decreased Na+flux in polarized taste buds via amiloride-sensitive and amiloride-insensitive Na+transport systems. The speed and partial amiloride-sensitivity of these changes in Na+flux indicate that IL-1β and TNF-α modulate epithelial Na+channel (ENaC) function. A portion of the TNF-mediated decrease in Na+flux is also blocked by the TRPV1 antagonist, capsazepine, though TNF-α further reduced Na+transport independently of both amiloride and capsazepine.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related TRP Channel Products

CAS 1024448-59-6 RN 1747

RN 1747
(CAS: 1024448-59-6)

RN 1747, a selective TRPV4 agonist (EC50= 0.77, 4.0 and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively), represents the first drug-like TRPV4 antagonist with...

(CAS: 1332708-14-1)

PF-4840154 has been foundd to be superior than Mustard Oil as a TrpA1 agonists. IC50: 97 nM and 23 nM (EC50) for hTrpA1 and rTrpA1 respectively.

CAS 1333210-07-3 SAR7334

(CAS: 1333210-07-3)

SAR7334, a TRPC6 inhibitor, could be valuable in studying sorts of diseases related to TRPC.

CAS 659730-32-2 AMG-517

(CAS: 659730-32-2)

AMG-517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM.

CAS 821768-06-3 JNJ-17203212

(CAS: 821768-06-3)

JNJ-17203212 is a novel, reversible, and selective TRPV1 antagonist which could not inhibit related TRP channels. Its IC50 values are 65 nM and 102 nM for human...

(CAS: 245747-08-4)

Pyr6, a pyrazole derivative, is a selective inhibitor of ransient receptor potential cation 3 (TRPC3) channels that inhibited Orai1- and TRPC3-mediated Ca(2+) e...

(CAS: 878811-00-8)

MK-2295 is a potent TRPV1 antagonist. TRPV1 antagonists has the potential as analgesic and anti-inflammatory agents.

CAS 1221349-53-6 TC-I 2014

TC-I 2014
(CAS: 1221349-53-6)

TC-I 2014 is a potent TRPM8 antagonist (IC50 = 0.8, 3.0 and 4.4 nM for canine, human and rat channels, respectively) displaying antiallodynic properties in vivo...

CAS 1160514-60-2 Pyr3

(CAS: 1160514-60-2)

Pyr3, a pyrazole derivative, is a selective antagonist of the TRP canonical 3 channel (TRPC3) which can function as a receptor-operated channel. It inhibits TRP...

CAS 461000-66-8 Eact

(CAS: 461000-66-8)

Eact is a TMEM16A (ANO1) calcium-activated chloride channel (CaCC) activator (EC50 = 3 μM). Eact also stimulates transient receptor potential vanilloid 1 (TRPV1...

CAS 1031496-06-6 CIM 0216

CIM 0216
(CAS: 1031496-06-6)

CIM 0216 has been found to be a selective TRPM3 agonist and could stimulate the release of insulin from pancreatic islet cells.

(CAS: 1315323-00-2)

Pyr10, a pyrazole derivative, is a TRPC3-selective inhibitor that could be effective in the study of cellular functions. IC50: 0.72 uM and 13.08 uM for TRPC3-RO...

CAS 1062271-24-2 MK6-83

(CAS: 1062271-24-2)

MK6-83 is a transient receptor potential channel ML3 activator with EC50 value of 110 nM. It can restore endolysosomal trafficking and zinc homeostasis in lysos...

CAS 332382-54-4 ML SA1

(CAS: 332382-54-4)

ML SA1 is an activator of TRPML channels. It can induce TRPML-mediated Ca2+ release from lysosomes and reduce cholesterol accumulation in Niemann-Pick type C ma...

CAS 459429-39-1 SB 452533

SB 452533
(CAS: 459429-39-1)

SB 452533 is a potent and selective TRPV1 antagonist against capsaicin (pKb = 7.7), noxious heat and acid-mediated (pIC50 = 7.0) receptor activation (pKi = 6.22...

(CAS: 956274-94-5)

Mavatrep is an orally bioavailable, potent and selective TRPV1 antagonist with Ki value of 6.5 nM, which exhibits minimal effect on the enzymatic activity of CY...

CAS 1883711-97-4 AM 0902

AM 0902
(CAS: 1883711-97-4)

AM 0902 is an effective and selective TRPA1 antagonist and has been found to exhibit activities in biological pathways associated with pain.

CAS 348575-88-2 Optovin

(CAS: 348575-88-2)

Optovin is a reversible photoactive TRPA1 activator; stimulates human TRPA1 channels in vitro and enables repeated photoactivation of motor behaviors in wild-ty...

CAS 883976-12-3 M8 B hydrochloride

M8 B hydrochloride
(CAS: 883976-12-3)

M8 B hydrochloride is a selective and potent channel blocker of transient receptor potential melastatin 8 (TRPM8). It blocks cold-induced and icilin or methol-i...

CAS 105955-11-1 OLDA

(CAS: 105955-11-1)

OLDA is a vanilloid TRPV1 (VR1) receptor agonist with EC50 value of 36 nM at hVR1. OLDA is also a 5-lipoxygenase inhibitor with IC50 value of 7.5 nM.

Chemical Structure

CAS 138977-28-3 Capsazepine

Quick Inquiry

Verification code

Featured Items