Cat. No.: HY-108482

CP-96,345

Name: CP-96,345
Brand: MedChemExpress
SKU: HY-108482
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CP-96,345 is a non-peptide selective NK-1 receptor antagonist (K_i = 0.31 nM). CP-96,345 inhibits cell rolling, adhesion, and plasma extravasation, and inhibits degranulation and pancreatic MPO activity. CP-96,345 attenuates neurogenic inflammation, edema, and adhesion molecule expression. CP-96,345 attenuates static contraction- and muscle stretch-evoked pressor reflexes through blockade of NK-1 receptors in the dorsal horn. CP-96,345 impairs post-ischemic recovery of LVDevP, HR, and CF in isolated hearts and increases reperfusion fibrillation. CP-96,345 can be used for research on chronic colitis, myocardial ischemia-reperfusion injury, smoke inhalation and burn injury, acute pancreatitis, oxazolone colitis, and neurogenic inflammation.

For research use only. We do not sell to patients.

Purity : 99.9%
CAS No.: 132746-60-2
Formula: C₂₈H₃₂N₂O
Molecular Weight:412.57

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

CP-96,345 Chemical Structure

CAS No.: 132746-60-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Protocols (4)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

NK1R

0.31 nM (Ki)

All Neurokinin Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	46.83 μM Compound: CP-96345	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 28710964]
CHO	IC₅₀	0.45 nM Compound: CP-96345	Binding affinity against human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P. Binding affinity against human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.	[PMID: 7535362]
CHO	IC₅₀	0.5 nM Compound: CP-96345	Binding affinity against wild type human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P. Binding affinity against wild type human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.	[PMID: 7535362]
CHO	IC₅₀	22 nM Compound: CP-96345	Binding affinity against Gln165Ala mutant type human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P. Binding affinity against Gln165Ala mutant type human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.	[PMID: 7535362]
CHO	IC₅₀	0.2 nM Compound: 1, (CP-96345)	Tested against cloned human NK1 receptor by displacement of 125 I -labeled substance P expressed in CHO cells Tested against cloned human NK1 receptor by displacement of 125 I -labeled substance P expressed in CHO cells	[PMID: 8393115]
CHO	IC₅₀	0.4 nM Compound: 2	Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells	[PMID: 8627597]
CHO	IC₅₀	0.5 nM Compound: CP-96345	Inhibition of [125I]-substance P binding to human neurokinin-1 (hNK-1) receptor in CHO cells Inhibition of [125I]-substance P binding to human neurokinin-1 (hNK-1) receptor in CHO cells	10.1016/0960-894X(95)00080-D
CHO	IC₅₀	0.7 nM Compound: CP-96345	Compound was tested for the displacement of [ 1251] Substance P from hNK1 receptor in CHO cells Compound was tested for the displacement of [ 1251] Substance P from hNK1 receptor in CHO cells	10.1016/S0960-894X(01)80280-8
CHO	IC₅₀	0.5 nM Compound: 1	Inhibition of [125I]-Substance P binding to human NK1 receptors in CHO cells Inhibition of [125I]-Substance P binding to human NK1 receptors in CHO cells	10.1016/S0960-894X(01)80747-2
IM-9	IC₅₀	0.77 nM Compound: 3, (CP-96345)	Binding affinity towards Tachykinin receptor 1 in human IM-9 cells using [3H]-substance P as ligand Binding affinity towards Tachykinin receptor 1 in human IM-9 cells using [3H]-substance P as ligand	[PMID: 1378901]
IM-9	IC₅₀	0.48 nM Compound: 1	Tested in vitro for the binding affinity towards NK1 receptor in human IM-9 cells using [125I]-labeled bolton-hunter substance P as ligand Tested in vitro for the binding affinity towards NK1 receptor in human IM-9 cells using [125I]-labeled bolton-hunter substance P as ligand	[PMID: 7520943]
IM-9	IC₅₀	0.35 nM Compound: 1	Inhibitory activity against Tachykinin receptor 1 in human IM-9 cells using [125I]-labeled Boltan-Hunter substance P as radioligand Inhibitory activity against Tachykinin receptor 1 in human IM-9 cells using [125I]-labeled Boltan-Hunter substance P as radioligand	[PMID: 8576917]
IM-9	IC₅₀	0.33 nM Compound: CP-96345	Binding affinity against Neurokinin 1(NK1) receptor from human IM-9 cells using [I]-Bolton Hunter labeled SP Binding affinity against Neurokinin 1(NK1) receptor from human IM-9 cells using [I]-Bolton Hunter labeled SP	10.1016/0960-894X(96)00148-5
IM-9	IC₅₀	4.2 nM Compound: CP-96345	Compound was evaluated for the inhibition of binding of [3H]SP in human IM-9 cells Compound was evaluated for the inhibition of binding of [3H]SP in human IM-9 cells	10.1016/S0960-894X(00)80693-9
IM-9	IC₅₀	0.52 nM Compound: CP-96345	Compound was tested in vitro for its Tachykinin receptor 1 affinity by the displacement of [125I]Bolton-Hunter substance p from human IM-9 cells Compound was tested in vitro for its Tachykinin receptor 1 affinity by the displacement of [125I]Bolton-Hunter substance p from human IM-9 cells	10.1016/S0960-894X(01)80246-8
IM-9	IC₅₀	2 nM Compound: CP-96345	Inhibitory concentration for displacement of [3H]-Substance P (SP) in human IM-9 cells Inhibitory concentration for displacement of [3H]-Substance P (SP) in human IM-9 cells	10.1016/S0960-894X(01)80859-3
MRC5	IC₅₀	57.9 μM Compound: CP-96345	Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay	[PMID: 28710964]
U-373MG ATCC	IC₅₀	9 nM Compound: 1, (CP-96345)	Compound was tested for inhibition of substance P induced phosphatidyl inositol turnover in human U-373 cells Compound was tested for inhibition of substance P induced phosphatidyl inositol turnover in human U-373 cells	10.1016/0960-894X(96)00287-9

In Vitro

CP-96,345 (0.1 μM; 5 days) inhibits intestinal antigen-stimulated proliferation of CD4⁺CD25^- T cells from BALB/c mice and, to a lesser extent, the proliferation of CD4⁺ T cells from colitic SCID mice^[1].
CP-96,345 (0.01 mM; 1 h) completely inhibits neurotensin-mediated mast cell degranulation in rat colonic explants, indicating that colonic mast cell activation in response to neurotensin involves substance P release^[8].
CP-96,345 (1 μM) abolishes the beneficial effects of SP on post-ischemic recovery of ischemic contracture, LVDevP, HR, and CF, reduces the anti-fibrillatory effect of SP, and prevents the SP-mediated decrease in CK release in isolated perfused rat hearts, whereas CP-96,345 alone impairs post-ischemic recovery (LVDevP is 39% of the pre-ischemic level)^[3].
CP-96,345 (1-100 nM; 15 min) competitively antagonizes Substance P (HY-P0201)-induced relaxation in noradrenaline-precontracted rabbit aortic rings, with a pA₂ of 8.15^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

CP 96,345 (1 µg/g; subcutaneous injection; three times per week; 8 weeks) attenuates mucosal inflammation in T cell transfer colitis, reducing the median colitis score to 3, but does not prevent weight loss^[1].
CP 96,345 (10 mg/kg; i.v.; 1 h before injury and every 12 h; 48 h) attenuates lung injury and inflammation in SB-injured mice, significantly reducing Evans blue extravasation by 31%, wet/dry weight ratio by 23%, hemoglobin by 46%, and myeloperoxidase activity by 54%^[4].
CP-96,345 (2.5 mg/kg; i.p.; single dose; 30 min before or 1 h after the first caerulein injection) effectively reduces the expression of adhesion molecules and leukocyte recruitment in the pancreas and lung in caerulein (HY-A0190)-induced acute pancreatitis in mice^[5].
CP-96345 (2.5 μg/g; i.p.; twice daily; 4 days) abolishes Oxazolone (HY-126360) colitis in CGRP^−/− mice^[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

SCID mice (female, 6-8 weeks old, T-cell transfer model)^[1]
Dosage:

1 µg/g
Administration:

s.c.; three times a week; 8 weeks
Result:

Reduced the median colitis inflammatory score to 3 compared to 5 in the control group.
Did not prevent body weight loss.

Animal Model:

C57BL/6 (male, 5-6 weeks old, 19-21 g, smoke inhalation and burn injury)^[4]
Dosage:

10 mg/kg
Administration:

i.v.; 1 hr prior to injury and every 12 hours; 48 hr
Result:

Decreased Evans Blue levels by 31%.
Decreased wet/dry weight ratio by 23%.
Decreased hemoglobin levels by 46%.
Decreased myeloperoxidase activity by 54%.
Showed higher Evans Blue levels (110%) compared to sham animals.
Showed higher hemoglobin levels (14%) compared to sham animals.

Animal Model:

Balb/C (Male, 20-25 g)^[5]
Dosage:

2.5 mg/kg
Administration:

i.p.; single dose; 30 min before or 1 h after first caerulein injection
Result:

Reduced plasma amylase levels and pancreatic water content.
Reduced pancreatic MPO activity.
Reduced protein immunoreactivity of ICAM-1 and VCAM-1 in pancreas.
Reduced mRNA and protein expression of E-selectin and P-selectin in pancreas.
Suppressed elevated ICAM-1, E-selectin, and P-selectin mRNA expression in lungs.
Reduced rolling leukocyte flux to 102.00 cells/min (prophylactic) and 132.75 cells/min (therapeutic).
Reduced adherent leukocytes to 3.67 cells/100 μm (prophylactic) and 4.67 cells/100 μm (therapeutic).
Restored rolling velocity to 25.32 μm/s (prophylactic) and 23.88 μm/s (therapeutic).
Suppressed proinflammatory leukocyte behaviors by approximately 50%.

Chemical Information

CAS No. 132746-60-2
Appearance Solid
Molecular Weight 412.57
Formula C₂₈H₃₂N₂O
Color White to light yellow
SMILES

COC1=C(C=CC=C1)CN[C@@H]2[C@@H](N3CCC2CC3)C(C4=CC=CC=C4)C5=CC=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Protocols

All Molecular Biology Animals and Diseases Signal Pathway Related

RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
DSS-Induced Colitis
Dextran sulfate sodium (DSS)-induced colitis is generated by administering DSS in mouse drinking water, producing epithelial injury, barrier disruption, weight loss, diarrhea, fecal blood, colon shortening, histologic mucosal damage, and inflammatory mediator changes; the model is mainly used to study acute or chronic intestinal inflammation resembling selected features of ulcerative colitis. DSS injury is interpreted through clinical and tissue readouts rather than a single molecular endpoint: daily body weight, stool consistency, and bleeding are combined into a disease activity index, while colon length, histology, cytokines, myeloperoxidase activity, intestinal permeability, and tight-junction markers provide complementary measures of inflammation and barrier damage.
TNBS-Induced Colitis
TNBS-induced colitis is produced by intrarectal delivery of 2,4,6-trinitrobenzene sulfonic acid in ethanol, where ethanol disrupts the mucosal barrier and TNBS haptenates colonic proteins, generating immune-mediated colonic inflammation with weight loss, diarrhea, ulceration, transmural injury, inflammatory-cell infiltration, and cytokine responses. The model is used as an experimental intestinal inflammation model with Crohn’s disease–like features, especially when Th1-type responses, IL-12–dependent inflammation, chronic relapsing inflammation, or fibrosis-related endpoints are studied.
Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (540 KB)
- English - EN (540 KB)
- Français - FR (540 KB)
- Deutsch - DE (540 KB)
- Norwegian - NO (540 KB)
- Español - ES (540 KB)
- Swedish - SV (540 KB)
- Italian - IT (540 KB)
- Korean - KR (540 KB)
- Portuguese - PT (540 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Gad M, et al. Blockage of the neurokinin 1 receptor and capsaicin-induced ablation of the enteric afferent nerves protect SCID mice against T-cell-induced chronic colitis. Inflammatory bowel diseases. 2009 Aug;15(8):1174-82.

[2]. Wilson LB, et al. Segmental effect of spinal NK-1 receptor blockade on the pressor reflex. American Journal of Physiology-Heart and Circulatory Physiology. 1998 Sep 1;275(3):H789-96.

[3]. Ustinova EE, et al. Neuropeptide depletion impairs postischemic recovery of the isolated rat heart: role of substance P. Cardiovascular research. 1995 Jul;30(1):55-63.

[4]. Jacob S, et al. Substance P antagonist CP-96345 blocks lung vascular leakage and inflammation more effectively than its stereoisomer CP-96344 in a mouse model of smoke inhalation and burn injury. Toxicology mechanisms and methods. 2010 May;20(4):197-203.

[5]. Lau HY, et al. Effect of CP-96,345 on the expression of adhesion molecules in acute pancreatitis in mice. American journal of physiology. Gastrointestinal and liver physiology. 2007 May;292(5):G1283-92.

[6]. Rubino A, et al. Endothelium-dependent relaxant effect of neurokinins on rabbit aorta is mediated by the NK1 receptor. European journal of pharmacology. 1992 Mar 03;212(2-3):237-40.

[7]. Engel MA, et al. Opposite effects of substance P and calcitonin gene-related peptide in oxazolone colitis. Digestive and liver disease : official journal of the Italian Society of Gastroenterology and the Italian Association for the Study of the Liver. 2012 Jan;44(1):24-9.

[8]. Castagliuolo I, et al. Neurotensin is a proinflammatory neuropeptide in colonic inflammation. The Journal of clinical investigation. 1999 Mar;103(6):843-9.

[9]. Baluk P, et al. NK1 receptors mediate leukocyte adhesion in neurogenic inflammation in the rat trachea. Am J Physiol. 1995 Feb;268(2 Pt 1):L263-9.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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CP-96,345

All Neurokinin Receptor Isoforms