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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
61 Results for "
H4 receptor
" in MedChemExpress (MCE) Product Catalog:
Products (61)
61 Results for "H4 receptor" in MCE Product Catalog:
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Adriforant hydrochloride (PF-3893787 hydrochloride) is a novel histamine H4 receptor antagonist binding affinity (Ki=2.4 nM) and is also a functional (Ki=1.56 nM) antagonist.
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1 Cited Publications
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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 .
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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 .
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Cat. No.: HY-P99242
CAS No.: 2254029-91-7
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Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits GABA receptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
Synonyms: VUF 8325 dihydrobromide; SKF 91105 dihydrobromide
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Imetit dihydrobromide (VUF 8325 dihydrobromide) is a high affinity and potent agonist of histamine H3 and H4 receptors, with Ki values of 0.3 and 2.7 nM, respectively. Imetit mimics histamine effect in triggering a shape change in eosinophils (EC50=25 nM) .
Cat. No.: HY-16756
CAS No.: 952494-46-1
Synonyms: JNJ-38518168
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Toreforant is a potent and selective histamine H4 receptor (H4R) antagonist, with a Ki at the human receptor of 8.4 nM.
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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 .
Synonyms: JW1601
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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 .
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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 Ki 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 .
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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 (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM) . Clobenpropit dihydrobromide increases apoptosis .
Synonyms: VUF6002
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JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively .
Synonyms: SENS-111
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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 .
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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 .
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VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.
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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 .
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H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.
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VUF 8430 (dihydrobromide) is a potent and selective histamine H4 receptor agonist with a Ki of 31.6 nM and an EC50 of 50 nM .
Cat. No.: HY-113936
CAS No.: 1027330-97-7
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A-943931 is a potent and selective histamine H4 receptor (H4R) antagonist with pKi values of 4.6, 3.8 nM for human and rat H4R, respectively. A-943931 shows anti-inflammatory and antinociceptive efficacy .
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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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
