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pA2 value

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (7) Adrenergic Receptor (8) Angiotensin Receptor (2) Bacterial (1) Cholinesterase (ChE) (1) Dopamine Receptor (2) Endogenous Metabolite (2) Histamine Receptor (9) iGluR (1) Isotope-Labeled Compounds (4) Leukotriene Receptor (1) mAChR (1) Neurokinin Receptor (1) Neuropeptide S Receptor (1) Prostaglandin Receptor (1) Reference Standards (4) SARS-CoV (1)
By Research Areas:	Cancer (6) Cardiovascular Disease (4) Endocrinology (5) Infection (1) Inflammation/Immunology (4) Metabolic Disease (7) Neurological Disease (15)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0693

Ranitidine 3 Publications Verification	Histamine Receptor	Metabolic Disease Cancer
Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with *pA₂* values of 7.2 and 6.95, respectively. Ranitidine inhibits breast tumor development and spread in mice .

HY-10349

WAY-100635 Maximum Cited Publications 12 Publications Verification	5-HT Receptor Dopamine Receptor	Neurological Disease
WAY-100635 is a potent and selective 5-HT_1A Receptor antagonist with a pIC₅₀ of 8.87, an apparent pA₂ of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC₅₀ value of 0.91 nM and K_i value of 0.39 nM. WAY-100635 has pIC₅₀ values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D₄ receptor agonist .

HY-B0281A

Ranitidine hydrochloride 3 Publications Verification	Histamine Receptor	Metabolic Disease Cancer
Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with *pA₂* values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice .

HY-108626

ML154 NCGC84	Neuropeptide S Receptor	Neurological Disease
ML154 (NCGC84) is a selective, brain-penetrant and non-peptide neuropeptide S receptor (NPSR) antagonist with a *pA₂* of 9.98. ML154 potently inhibits NPS-stimulated cellular calcium, cAMP, and ERK phosphorylation responses with IC₅₀ values of 36.5 nM, 22.1 nM, and 9.3 nM, respectively .

HY-101336

RS 17053 hydrochloride RS-17053	Adrenergic Receptor	Metabolic Disease Endocrinology
RS 17053 hydrochloride is a potent and selective α1_A adrenoceptor antagonist, with a pK_i value of 9.1 in native cell membrane and a *pA₂* value of 9.8 in functional assays.

HY-151413

MEN 10207 1 Publications Verification	Neurokinin Receptor	Neurological Disease
MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.

HY-B0693A

Ranitidine bismuth citrate	Histamine Receptor SARS-CoV Bacterial	Infection Metabolic Disease Cancer
Ranitidine bismuth citrate is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine bismuth citrate antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with *pA₂* values of 7.2 and 6.95, respectively. Ranitidine bismuth citrate has selectivity for SARS-CoV-2-infected cells. Ranitidine bismuth citrate also has anti-Helicobacter pylori infection. Ranitidine bismuth citrate inhibits breast tumor development and spread in mice .

HY-19432

UBP-282	iGluR	Neurological Disease
UBP-282 is a potent, selective and competitive AMPA and kainate receptor antagonist. UBP-282 inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC₅₀ value of 10.3 μM. UBP-282 antagonizes kainate-induced depolarisations of dorsal roots with a *pA₂* value of 4.96 .

HY-10382

EXP-6803	Angiotensin Receptor	Cardiovascular Disease
EXP-6803 is a specific nonpeptide angiotensin II receptor antagonist with antihypertensive activity. EXP-6803 inhibits the contractile response to angiotensin II with a pA₂ value of 7.20. EXP-6803 effectively blocks responses to angiotensin I and II while not affecting responses to bradykinin or acetylcholine in guinea pig ileum. EXP-6803 can be used for hypertension research .

HY-121603

Bornaprine	Cholinesterase (ChE)	Neurological Disease
Bornaprine is an anticholinergic agent that can be used in the study of parkinsonism. Bornaprine shows a pA2 value of 7.27 .

HY-139045

2,4-DMA hydrochloride	5-HT Receptor	Neurological Disease
2,4-DMA hydrochloride is an amphetamine and is a serotonin 5-HT2 receptor agonist with an apparent *PA₂* value of 5.6 .

HY-U00355

YM158 free base YM-57158	Leukotriene Receptor Prostaglandin Receptor	Inflammation/Immunology Endocrinology
YM158 free base is a potent and selective LTD₄ and TXA₂ receptor antagonist with *pA₂* values of about 8.87 and 8.81, respectively.

HY-W713312

2,6-DMA hydrochloride	5-HT Receptor	Neurological Disease
2,6-DMA hydrochloride is classified as an amphetamine. 2,6-DMA hydrochloride is a serotonin 5-HT2 receptor agonist with an apparent pA2 value of 5.09.

HY-119262

ABT-866	Adrenergic Receptor	Cardiovascular Disease Endocrinology
ABT-866 is an α_1A-adrenoceptor agonist and an antagonist at the α_1B- and α_1D-adrenoceptor subtypes. ABT-866 has an EC₅₀ of 0.60 μM for the α_1A in the rabbit urethra. ABT-866 has a *pA₂* value of 5.4 for the α_1B in the rat spleen. ABT-866 has a *pA₂* value of 6.2 for the α_1D in the rat aorta. ABT-866 exhibits good urethral selectivity and lower cardiovascular side effects in stress urinary incontinence models. ABT-866 can be used for the research of diseases such as stress urinary incontinence .

HY-U00079A

Vamicamide FK-176	mAChR	Neurological Disease
Vamicamide (FK-176) is an orally active competitive mAChR antagonist that inhibits contractions induced by cholinergic nerve stimulation by preventing mAChR agonists from binding to mAChR. Vamicamide exhibits a good anti-bladder spasm effect, with a *pA2* value of 6.82 in bladder tissue. Vamicamide can be used in research within the field of neurological diseases .

HY-107748A

5'-Guanidinonaltrindole TFA 5'-GNTI TFA	Endogenous Metabolite	Neurological Disease
5'-Guanidinonaltrindole TFA is a selective kappa-opioid receptor antagonist with significant opioid antagonist activity. 5'-Guanidinonaltrindole TFA exhibits 5 times the antagonistic potency of the prototypical kappa-opioid receptor antagonist norbinatorphimine in smooth muscle preparations, with a selectivity ratio exceeding 500 times. Binding and functional studies of 5'-Guanidinonaltrindole TFA showed pA(2) values comparable to smooth muscle data. 5'-Guanidinonaltrindole TFA is regarded as a potentially valuable pharmacological tool for studying opioids due to its high selectivity and potency .

HY-107564

Impentamine dihydrobromide VUF 4702 dihydrobromide	Histamine Receptor	Inflammation/Immunology
Impentamine dihydrobromide (VUF 4702 dihydrobromide) is a histamine H3 receptor antagonist with potential antihistamine activity. Impentamine dihydrobromide shows the strongest selective H3 antagonism among a series of 4(5)-(ω-aminoalkyl)-1H-imidazole compounds. The pA2 value of impentamine dihydrobromide is 8.4, showing its high efficacy in guinea pig jejunum. Impentamine dihydrobromide has a specific antagonistic binding site with the H3 receptor .

HY-101823A

A-81282 Abbott 81282	Angiotensin Receptor	Cardiovascular Disease
A-81282 (Abbott 81282) is an antagonist of angiotensin II's AT1 receptor, with a *p_A2* value of 9.64 at the AT1 receptor in rabbit aorta. A-81282 also demonstrates significant inhibitory action on the binding of [125i]_Sar1_lle8_Angiotensin_ll to rat liver membranes, with a p_KI value of 8.505. A-81282 has antihypertensive activity and can effectively lower blood pressure in renal artery-ligated rats .

HY-100634S

4-Hydroxypropranolol-d7 hydrochloride (±)-4-Hydroxy Propranolol-d7 hydrochloride	Isotope-Labeled Compounds Adrenergic Receptor	Neurological Disease
4-Hydroxypropranolol-d₇ (hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties .

HY-B0281AS

Ranitidine-d6 hydrochloride	Isotope-Labeled Compounds Histamine Receptor	Metabolic Disease Cancer
Ranitidine-d₆ hydrochloride is the deuterium labeled Ranitidine hydrochloride (HY-B0281A) . Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with *pA₂* values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice .

HY-100634SA

4-Hydroxypropranolol-d7 (±)-4-Hydroxy Propranolol-d₇	Isotope-Labeled Compounds Adrenergic Receptor	Neurological Disease
4-Hydroxypropranolol-d₇ is the deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties .

HY-B0693S

Ranitidine-d6	Isotope-Labeled Compounds Histamine Receptor	Cancer
Ranitidine-d₆ is the deuterium labeled Ranitidine (HY-B0693). Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine inhibits breast tumor development and spread in mice .

HY-B0281AR

Ranitidine hydrochloride (Standard)	Reference Standards Histamine Receptor	Metabolic Disease Cancer
Ranitidine hydrochloride (Standard) is the analytical standard of Ranitidine hydrochloride (HY-B0281A). This product is intended for research and analytical applications. Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with *pA₂* values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice.

HY-100634R

4-Hydroxypropranolol hydrochloride (Standard) (±)-4-hydroxy Propranolol hydrochloride (Standard)	Reference Standards Adrenergic Receptor	Neurological Disease
4-Hydroxypropranolol (hydrochloride) (Standard) is the analytical standard of 4-Hydroxypropranolol (hydrochloride). This product is intended for research and analytical applications. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties .

HY-117063

LEK 8841 methanesulfonate	5-HT Receptor	Endocrinology
LEK 8841 methanesulfonate is a gastrointestinal calming agent with strong selective 5-HT2 receptor antagonist activity. The antipsychotic potential of LEK 8841 has made it the focus of research into alternative medicines. LEK 8841 behaves as a pure competitive antagonist in response to 5-HT and norepinephrine, with pA2 values of 7.93 and 6.45, respectively. The selectivity of LEK 8841 is better than that of the comparative drug ketanserin, making it an important reference value in corresponding receptor research. Studies related to structural modifications have shown that LEK 8841 exhibits high affinity for 5-HT2 receptors and low alpha-adrenergic receptor activity .

HY-119854

Atiprosine AY-28228	Adrenergic Receptor 5-HT Receptor Histamine Receptor	Cardiovascular Disease Neurological Disease
Atiprosine (AY-28228) is an orally effective selective α1-adrenergic receptor antagonist with a *pA₂* value of 8.11. Atiprosine exhibits antagonistic activity against α2-adrenergic receptors (α1-adrenergic receptor), 5-HT₂ receptors (5-HT₂ receptor), and H₁ receptors (H₁ receptor). The *pA₂* values for these receptors are 6.04, 6.87, and 7.32 respectively. Atiprosine has antihypertensive and hypotensive effects in rats, dogs, and monkeys. It can be used for research on cardiovascular and mental disorders.

HY-10349R

WAY-100635 (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor	Neurological Disease
WAY-100635 (Standard) is the analytical standard of WAY-100635. This product is intended for research and analytical applications. WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist .

HY-136693

L-654284	Adrenergic Receptor	Neurological Disease
L-654284 is an α2-adrenergic receptor antagonist with significant selectivity. L-654284 competes with the binding of 3H-clonidine and 3H-rauwolscine in vitro and shows K_i values of 0.8 nM and 1.1 nM, respectively. L-654284 can block the protrusion effect of clonidine in isolated vas deferens in rats, with a pA2 value of 9.1. L-654284 exhibits remarkable selectivity for α2 and α1 adrenergic receptors, and exhibits a K_i of 110 nM in inhibiting 3H-prazosin binding. L-654284 can significantly increase the turnover rate of norepinephrine in rat cerebral cortex in vivo, showing α2-adrenergic receptor blocking activity in the central nervous system .

HY-101336R

RS 17053 hydrochloride (Standard) RS-17053 (Standard)	Adrenergic Receptor Reference Standards	Metabolic Disease Endocrinology
RS 17053 hydrochloride (Standard) is the analytical standard of RS 17053 hydrochloride (HY-101336). This product is intended for research and analytical applications. RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.

HY-120053

SC-53606	5-HT Receptor	Inflammation/Immunology
SC-53606 is a potent and selective 5-HT₄ receptor antagonist, with a *pA2* value of 8.13. SC-53606 acts as an antagonist of 5-HT₄ receptor-mediated relaxation of Carbachol (HY-B1208)-induced contractions .

HY-182393

IGN-2098	Histamine Receptor	Inflammation/Immunology
IGN-2098 is an orally active, competitive histamine H₂receptor antagonist with a *pA₂* value of 7.32. IGN-2098 inhibits basal and stimulated gastric acid secretion. IGN-2098 accelerates ulcer healing, suppresses ulcer edge elevation, and protects gastric and duodenal mucosa from damage. IGN-2098 can be used in research related to gastric ulcers .

HY-103294

R892	Endogenous Metabolite	Others
R892 is a selective and efficient bradyK_inin B1 receptor antagonist with significant antagonistic activity. The pA2 values of R892 in human and rabbit B1 receptors are 8.8 and 8.6 respectively, indicating its strong anti-activity at these receptors. R892 exhibits selectivity with ID50 values of 2.8 nM and >600 nM for B1 and B2 receptors, respectively, and has no endogenous agonist activity. R892 is resistant to aminopeptidase and kininase II (ACE) degradation and exhibits metabolic stability .

Cat. No.	Product Name	Target	Research Area

HY-151413

MEN 10207 1 Publications Verification	Neurokinin Receptor	Neurological Disease
MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.

HY-103294

R892	Endogenous Metabolite	Others
R892 is a selective and efficient bradyK_inin B1 receptor antagonist with significant antagonistic activity. The pA2 values of R892 in human and rabbit B1 receptors are 8.8 and 8.6 respectively, indicating its strong anti-activity at these receptors. R892 exhibits selectivity with ID50 values of 2.8 nM and >600 nM for B1 and B2 receptors, respectively, and has no endogenous agonist activity. R892 is resistant to aminopeptidase and kininase II (ACE) degradation and exhibits metabolic stability .

Cat. No.	Product Name	Chemical Structure

HY-100634S

4-Hydroxypropranolol-d7 hydrochloride
4-Hydroxypropranolol-d₇ (hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties .

4-Hydroxypropranolol-d7 hydrochloride

4-Hydroxypropranolol-d₇ (hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties .

HY-B0281AS

Ranitidine-d6 hydrochloride
Ranitidine-d₆ hydrochloride is the deuterium labeled Ranitidine hydrochloride (HY-B0281A) . Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with *pA₂* values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice .

Ranitidine-d6 hydrochloride

Ranitidine-d₆ hydrochloride is the deuterium labeled Ranitidine hydrochloride (HY-B0281A) . Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA₂ values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice .

HY-100634SA

4-Hydroxypropranolol-d7
4-Hydroxypropranolol-d₇ is the deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties .

4-Hydroxypropranolol-d7

4-Hydroxypropranolol-d₇ is the deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties .

HY-B0693S

Ranitidine-d6
Ranitidine-d₆ is the deuterium labeled Ranitidine (HY-B0693). Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine inhibits breast tumor development and spread in mice .

Ranitidine-d6

Ranitidine-d₆ is the deuterium labeled Ranitidine (HY-B0693). Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine inhibits breast tumor development and spread in mice .

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