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Results for "

histamine H4 receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Histamine Receptor (48) Apoptosis (1) Drug Isomer (1) Isotope-Labeled Compounds (1) Reference Standards (5) STAT (1)
By Research Areas:	Cancer (6) Endocrinology (11) Infection (1) Inflammation/Immunology (33) Metabolic Disease (1) Neurological Disease (14)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: Histamine Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13508

JNJ-7777120 1 Publications Verification	Histamine Receptor	Inflammation/Immunology
JNJ-7777120 is a potent and selective **histamine H₄ receptor antagonist (K_i*=4.5 nM). JNJ-7777120 effectively blocks histamine*-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory .

HY-101173

Imetit dihydrobromide VUF 8325 dihydrobromide; SKF 91105 dihydrobromide	Histamine Receptor	Neurological Disease
Imetit dihydrobromide (VUF 8325 dihydrobromide) is a high affinity and potent agonist of histamine H3 and H4 receptors, with K_i values of 0.3 and 2.7 nM, respectively. Imetit mimics histamine effect in triggering a shape change in eosinophils (EC₅₀=25 nM) .

HY-16756

Toreforant JNJ-38518168	Histamine Receptor	Neurological Disease Endocrinology
Toreforant is a potent and selective histamine H₄ receptor (H4R) antagonist, with a K_i at the human receptor of 8.4 nM.

HY-101189

JNJ-39758979	Histamine Receptor	Neurological Disease Endocrinology
JNJ-39758979, a chemical probe, is a selective, orally active, and high-affinity **histamine H₄ receptor antagonist with K_i*s of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine* H₄ receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .

HY-17039

Alcaftadine 1 Publications Verification R89674	Histamine Receptor	Inflammation/Immunology Endocrinology
Alcaftadine (R89674) is a **histamine H1 receptor** antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis. Alcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. Alcaftadine also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects .

HY-107560

4-Methylhistamine dihydrochloride	Histamine Receptor	Inflammation/Immunology Cancer
4-Methylhistamine hydrochloride is the dihydrochloride salt of 4-Methylhistamine (HY-W580721). 4-Methylhistamine hydrochloride is a potent and selective agonist of **histamine 4 receptor** (H4R) with a K_i of 50 nM. 4-Methylhistamine hydrochloride has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine hydrochloride can potently activate the hH4R (pEC₅₀ = 7.4). 4-Methylhistamine hydrochloride can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation .

HY-147276

Izuforant JW1601	Histamine Receptor	Inflammation/Immunology
Izuforant (JW1601) (Compound 24) is an orally active histamine H4 receptor (H4R) antagonist with an IC₅₀ of 36 nM against human H4R. Izuforant also shows binding affinity of human serotonin 3 receptor (h5-HT3R) with an IC₅₀ of 9.1 μM. Izuforant exhibits strong anti-pruritic and anti-inflammatory efficacies .

HY-101198

Clobenpropit dihydrobromide	Histamine Receptor Apoptosis	Neurological Disease Cancer
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC₅₀ of 8.07 for histamine H3LR . Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (K_i 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (K_i 7.4 nM) and α2A/α2C adrenoceptors (K_i 17.4/7.8 nM) . Clobenpropit dihydrobromide increases apoptosis .

HY-109074

Seliforant SENS-111	Histamine Receptor	Neurological Disease
Seliforant (SENS-111) is a selective, orally active histamine H4 receptor antagonist. Seliforant inhibits the sustained activity of vestibular neurons and modulates vestibular-related responses. Seliforant reduces spontaneous nystagmus in rats with excitotoxic acute unilateral vestibular loss. Seliforant shows no sedative effect. Seliforant can be used in research related to acute unilateral vestibular loss, vestibular dysfunction, and acute unilateral vestibular lesions .

HY-123532

JNJ10191584 VUF6002	Histamine Receptor	Neurological Disease
JNJ10191584 (VUF6002) is an orally active and selective histamine H₄ receptor antagonist with a K_i value of 26 nM. JNJ10191584 shows 540-fold selectivity to H₄ receptor over H₃ receptor with a K_i value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC₅₀ values of 530 nM and 138 nM, respectively .

HY-19705B

Adriforant hydrochloride 2 Publications Verification PF-3893787 hydrochloride	Histamine Receptor	Inflammation/Immunology Endocrinology
Adriforant hydrochloride (PF-3893787 hydrochloride) is a novel **histamine H4 receptor antagonist binding affinity (K_i=2.4 nM) and is also a functional (K_i**=1.56 nM) antagonist.

HY-101063

Amthamine dihydrobromide	Histamine Receptor	Inflammation/Immunology
Amthamine is a histamine receptor (H1R-H4R) agonist. Amthamine can produce liver congestion and necrosis of liver cells. Amthamine can be used to study the induction effect of H1R-H4 agonist on hepatotoxicity .

HY-101420

VUF10460	Histamine Receptor	Inflammation/Immunology Endocrinology
VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pK_i of 7.46.

HY-101188

INCB38579	Histamine Receptor	Infection
INCB38579 is an orally active, highly brain penetrable, and selective histamine H₄ receptor (HH₄R) antagonist (hH₄R IC₅₀=4.8 nM, mH₄R IC₅₀=42 nM, rH₄R IC₅₀=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities .

HY-107555

VUF 8430 dihydrobromide	Histamine Receptor	Neurological Disease
VUF 8430 (dihydrobromide) is a potent and selective **histamine H4 receptor agonist with a K_i of 31.6 nM and an EC₅₀** of 50 nM .

HY-111501

H4R antagonist 1	Histamine Receptor	Inflammation/Immunology Endocrinology
H4R antagonist 1 is a potent and highly selective **histamine H4 receptor** (H4R) antagonist with an IC₅₀ of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R .

HY-113936

A-943931	Histamine Receptor	Neurological Disease Inflammation/Immunology
A-943931 is a potent and selective **histamine H4 receptor (H4R) antagonist with pK_i** values of 4.6, 3.8 nM for human and rat H4R, respectively. A-943931 shows anti-inflammatory and antinociceptive efficacy .

HY-145106

Histamine H4 receptor antagonist-1	Histamine Receptor	Inflammation/Immunology
Histamine H4 receptor antagonist-1 is an antagonist of **histamine H4 receptor** extracted from patent WO2010108059A1 compound 60 .

HY-115833

Histamine H4 receptor antagonist-2	Histamine Receptor	Cancer
Histamine H4 receptor antagonist-2 serves as a potent activator of p53, demonstrating significant antitumor efficacy.

HY-19705

Adriforant PF-3893787	Histamine Receptor	Inflammation/Immunology Endocrinology
PF-3893787 is a novel **histamine H4 receptor antagonist binding affinity (K_i=2.4 nM) and is also a functional (K_i**=1.56 nM) antagonist.

HY-129508

Amthamine	Histamine Receptor	Inflammation/Immunology
Amthamine is a histamine receptor (H1R-H4R) agonist. Amthamine can produce liver congestion and necrosis of liver cells. Amthamine can be used to study the induction effect of H1R-H4 agonist on hepatotoxicity .

HY-107561

A-943931 hydrochloride	Histamine Receptor	Inflammation/Immunology
A-943931 (Compound 10) is a histamine H₄ receptor antagonists. A-943931 has improved pharmacotropic and in vivo efficacy in models of pain and inflammation. A-943931 can be used in vivo anti-inflammatory and anti-nociception research .

HY-114025

H4 Receptor antagonist 1	Histamine Receptor	Neurological Disease Endocrinology
H4 Receptor antagonist 1 is a potent and selective **histamine H4 receptor inverse agonist, with an IC₅₀** of 19 nM.

HY-107558

JNJ10191584 maleate VUF6002 maleate	Histamine Receptor	Neurological Disease
JNJ10191584 (VUF6002) maleate (compound 40) is an orally active and selective histamine H₄ receptor antagonist with a K_i value of 26 nM. JNJ10191584 maleate shows 540-fold selectivity to H₄ receptor over the H₃ receptor with a K_i value of 14.1 μM. JNJ10191584 maleate inhibits chemotaxis of eosinophils and mast cells with IC₅₀ values of 530 nM and 138 nM, respectively .

HY-120541

ST-1006	Histamine Receptor	Inflammation/Immunology
ST-1006 is a potent **histamine H4 receptor agonist with a pK_i** value of 7.94. ST-1006 has anti-inflammatory effect .

HY-108977

VUF 8430	Histamine Receptor	Neurological Disease
VUF 8430 is a potent and selective **histamine H4 receptor agonist with a K_i of 31.6 nM and an EC₅₀** of 50 nM .

HY-120531

UR-PI376	Histamine Receptor	Neurological Disease
UR-PI376 is a potent and selective **histamine H4 receptor (H4R) agonist with a pEC₅₀** value of 7.47. UR-PI376 shows negligible hH1R and hH2R activities and moderate inverse agonistic activity at the hH3R .

HY-113669

A-940894	Histamine Receptor	Inflammation/Immunology
A-940894 is a potent **histamine H₄ receptor antagonist, with K_i** values of 7.6 nM (rat H₄) and 71 nM (human H₄). A-940894 exhibits with anti-inflammatory properties .

HY-118336

VUF10497	Histamine Receptor	Inflammation/Immunology
VUF10497 is a potent histamine H4 receptor (H4R) inverse agonist with anti-inflammatory activity .

HY-14845

Levomequitazine (S)-Mequitazine	Drug Isomer Histamine Receptor	Inflammation/Immunology
Levomequitazine (Compound V0114) ((S)-Mequitazine), the levorotatory enantiomer of Mequitazine (HY-B2168), is an orally active, inverse H4 receptor agonist (IC₅₀s: 94 nM (hM2), 17 nM (hM3)). Levomequitazine strongly binds to human histamine H4 receptor. Levomequitazine antagonizes the activating action induced by histamine on H4 receptor. Levomequitazine induces a powerful and statistically significant anti-inflammatory effect. Levomequitazine can be used for research on inflammatory diseases .

HY-101189B

JNJ-39758979 dihydrochloride	Histamine Receptor	Inflammation/Immunology
JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity **histamine H₄ receptor antagonist, with K_i*s of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine* H₄ receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity .

HY-120541A

ST-1006 Maleate	Histamine Receptor	Inflammation/Immunology
ST-1006 maleate is a potent **histamine H4 receptor agonist with a pK_i** value of 7.94. ST-1006 maleate has anti-inflammatory effect .

HY-W580721

4-Methylhistamine	Histamine Receptor	Inflammation/Immunology Cancer
4-Methylhistamine is a potent and selective agonist of **histamine 4 receptor** (H4R) with a K_i of 50 nM. 4-Methylhistamine has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine can potently activate the hH4R (pEC₅₀ = 7.4). 4-Methylhistamine can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation .

HY-17039R

Alcaftadine (Standard) R89674 (Standard)	Reference Standards Histamine Receptor	Inflammation/Immunology Endocrinology
Alcaftadine (Standard) is the analytical standard of Alcaftadine. This product is intended for research and analytical applications. Alcaftadine (R89674) is a **histamine H1 receptor** antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis. Alcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. Alcaftadine also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects .

HY-124356

Alcaftadine carboxylic acid	Histamine Receptor	Inflammation/Immunology
Alcaftadine carboxylic acid is a broad-spectrum antihistamine compound with high affinity for histamine H1 and H2 receptors and low affinity for H4 receptors. Alcaftadine carboxylic acid has also demonstrated effects on modulating immune cell recruitment and stabilizing mast cells. Alcaftadine carboxylic acid is more effective than placebo in preventing ocular itching associated with allergic conjunctivitis and is at least as effective as olopatadine 0.01% .

HY-124356AS

Alcaftadine carboxylic acid-d3 sodium	Isotope-Labeled Compounds Histamine Receptor	Inflammation/Immunology
Alcaftadine carboxylic acid-d₃ (sodium) is deuterium labeled Alcaftadine carboxylic acid. Alcaftadine carboxylic acid is a broad-spectrum antihistamine compound with high affinity for histamine H1 and H2 receptors and low affinity for H4 receptors. Alcaftadine carboxylic acid has also demonstrated effects on modulating immune cell recruitment and stabilizing mast cells. Alcaftadine carboxylic acid is more effective than placebo in preventing ocular itching associated with allergic conjunctivitis and is at least as effective as olopatadine 0.01% .

HY-13508R

JNJ-7777120 (Standard)	Histamine Receptor	Inflammation/Immunology
JNJ-7777120 (Standard) is the analytical standard of JNJ-7777120. This product is intended for research and analytical applications. JNJ-7777120 is a potent and selective histamine H4 receptor antagonist (Ki=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory .

HY-101420R

VUF10460 (Standard)	Histamine Receptor Reference Standards	Inflammation/Immunology Endocrinology
VUF10460 (Standard) is the analytical standard of VUF10460 (HY-101420). This product is intended for research and analytical applications. VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.

HY-117826

JNJ 28610244	Histamine Receptor	Inflammation/Immunology
JNJ 28610244 is a H4R agonist, with a pK_i of 7.3 and pEC₅₀ of 7.0, respectively .

HY-14364

A-987306	Histamine Receptor	Inflammation/Immunology
A-987306 is a potent and oral bioavailable histamine H₄ antagonist, with K_is of 3.4 nM and 5.8 nM for rat H₄, and human H₄. A-987306 shows anti-inflammatory activity in mice peritonitis model .

HY-113917

JNJ 40279486	Histamine Receptor	Inflammation/Immunology
JNJ 40279486 is a novel and highly selective **histamine H₄ receptor antagonist with a K_i** of 9 nM. JNJ 40279486 can be used in the research of immune-driven inflammatory diseases .

HY-156667

H4R antagonist 3	Histamine Receptor	Neurological Disease Metabolic Disease Inflammation/Immunology
H4R antagonist 3 (Example 8) is a **histamine-4 and -1 receptor antagonist with EC₅₀** of ≤10 mM. H4R antagonist 3 can be used for the research of prevention of inflammatory, autoimmune, allergic, and ocular diseases .

HY-109074R

Seliforant (Standard) SENS-111 (Standard)	Reference Standards Histamine Receptor	Inflammation/Immunology
Seliforant (Standard) is the analytical standard of Seliforant (HY-109074). This product is intended for research and analytical applications. Seliforant (SENS-111) is a selective and orally histamine H4 receptor antagonist.

HY-101189R

JNJ-39758979 (Standard)	Histamine Receptor Reference Standards	Neurological Disease Endocrinology
JNJ-39758979 (Standard) is the analytical standard of JNJ-39758979 (HY-101189). This product is intended for research and analytical applications. JNJ-39758979, a chemical probe, is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .

HY-122166

Histamine receptors inhibitor 1	STAT	Others
Histamine receptors inhibitor 1 (compound 303) is an inhibitor of H1R or H4R that can be used in the research of inflammatory, autoimmune, allergic, and ocular .

HY-W580721A

4-Methylhistamine hydrochloride	Histamine Receptor	Inflammation/Immunology Cancer
4-Methylhistamine hydrochloride is the hydrochloride salt of 4-Methylhistamine (HY-W580721). 4-Methylhistamine hydrochloride is a potent and selective agonist of **histamine 4 receptor** (H4R) with a K_i of 50 nM. 4-Methylhistamine hydrochloride has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine hydrochloride can potently activate the hH4R (pEC₅₀ = 7.4). 4-Methylhistamine hydrochloride can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation .

HY-165453

VUF14480	Histamine Receptor	Inflammation/Immunology
VUF14480 is a partial agonist of **histamine H4 (hH4) receptor**-mediated G protein signalling and β-arrestin2 recruitment. VUF14480 binds covalently to hH4 receptor (pK_i: 6.3 for hH4-WT receptor). VUF14480 partially induces hH4 receptor-mediated G protein activation and β-arrestin2 recruitment. VUF14480 can be used in the research of inflammatory diseases .

HY-124912

VUF-6884	Histamine Receptor	Others
VUF-6884 (Compound 7j) is a histamine receptor (Histamine *Receptor) ligand with activity toward human H4R* and H1R. Its pEC₅₀ and pK_i values against human *H4R* are 7.70 and 7.55, respectively, while those against human H1R are 8.17 and 8.11, respectively. VUF-6884 competitively binds to the orthosteric binding site of human *H4R* to displace histamine, and exhibits inverse agonist activity at human H1R .

HY-107560R

4-Methylhistamine dihydrochloride (Standard)	Reference Standards Histamine Receptor	Inflammation/Immunology Cancer
4-Methylhistamine dihydrochloride (Standard) is the analytical standard of 4-Methylhistamine (dihydrochloride) (HY-107560). This product is intended for research and analytical applications. 4-Methylhistamine hydrochloride is the dihydrochloride salt of 4-Methylhistamine (HY-W580721). 4-Methylhistamine hydrochloride is a potent and selective agonist of histamine 4 receptor (H4R) with a K_i of 50 nM. 4-Methylhistamine hydrochloride has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine hydrochloride can potently activate the hH4R (pEC₅₀ = 7.4). 4-Methylhistamine hydrochloride can be used for the researches of cancer, inflammation and immunology, such as lung cancer and sK_in inflammation .

Cat. No.	Product Name	Chemical Structure

HY-124356AS

Alcaftadine carboxylic acid-d3 sodium

Alcaftadine carboxylic acid-d₃ (sodium) is deuterium labeled Alcaftadine carboxylic acid. Alcaftadine carboxylic acid is a broad-spectrum antihistamine compound with high affinity for histamine H1 and H2 receptors and low affinity for H4 receptors. Alcaftadine carboxylic acid has also demonstrated effects on modulating immune cell recruitment and stabilizing mast cells. Alcaftadine carboxylic acid is more effective than placebo in preventing ocular itching associated with allergic conjunctivitis and is at least as effective as olopatadine 0.01% .

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