4 Results for "

Insurmountable antagonism

" in MedChemExpress (MCE) Product Catalog:
Products (4)

4 Results for "Insurmountable antagonism" in MCE Product Catalog:

Cat. No.: HY-124956
CAS No.: 957136-80-0
Research Areas:  

Metabolic Disease

GIV3727 is an orally active bitter taste receptor antagonist targeting TAS2R4, TAS2R7, TAS2R20, TAS2R31, TAS2R40, and TAS2R43, with orthosteric, insurmountable antagonism at hTAS2R31. GIV3727 blocks TAS2R4 and prevents Gallic acid-induced upregulation of GDF15 mRNA expression. GIV3727 inhibits agonist-evoked receptor activation. GIV3727 reduces the perceived bitterness of acesulfame K and saccharin without affecting sweet taste perception. GIV3727 can be used for obesity research .
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Cat. No.: HY-134971
CAS No.: 893426-98-7
Target:  

mAChR

Research Areas:  

Endocrinology

AE9C90CB is an M3 muscarinic receptor (mAChR) antagonist and M2 muscarinic receptor ligand (human pKi values of 9.9 and 8.6, respectively). AE9C90CB binds to the M3 receptor and produces an insurmountable antagonism of Carbamoylcholine chloride (HY-B1208)-induced bladder strip contraction, thereby inhibiting the elevation of intravesical pressure and salivation, and exhibits functional selectivity for the bladder relative to the salivary glands. AE9C90CB can be used in the study of overactive bladder .
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Cat. No.: HY-182635
CAS No.: 83812-65-1
ICI 147798 is an orally effective β-adrenoceptor antagonist with a pKB of 9.1 (in guinea pig right atrium) and 8.8 (in guinea pig trachea). ICI 147798 acts as a diuretic and intraocular pressure-lowering agent. ICI 147798 blocks β-adrenoceptors, inhibits isoproterenol-induced tachycardia and vasodepressor responses, exhibits slowly dissociating, insurmountable antagonism against β1-adrenoceptors, and shows surmountable competitive antagonism against β2-adrenoceptors. ICI 147798 induces natriuresis and kaliuresis, inhibits sodium transport, and reduces intraocular pressure .
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Cat. No.: HY-134971A
CAS No.: 893426-86-3
Target:  

mAChR

Research Areas:  

Endocrinology

AE9C90CB free base is an M3 muscarinic receptor (mAChR) antagonist and M2 muscarinic receptor ligand (human pKi values of 9.9 and 8.6, respectively). AE9C90CB binds to the M3 receptor and produces an insurmountable antagonism of Carbamoylcholine chloride (HY-B1208)-induced bladder strip contraction, thereby inhibiting the elevation of intravesical pressure and salivation, and exhibits functional selectivity for the bladder relative to the salivary glands. AE9C90CB can be used in the study of overactive bladder .
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