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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
60 Results for "
α1A‐adrenoceptor
" in MedChemExpress (MCE) Product Catalog:
Products (60)
60 Results for "α1A‐adrenoceptor" in MCE Product Catalog:
3
3 Cited Publications
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BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist [1] .
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Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) and 5-HT2A/5-HT1A receptor (Kis of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities [1] .
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Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia [1] .
1
1 Cited Publications
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Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
SB-699551 is a selective and brain penetrant 5-HT5A receptor antagonist with a pKi of 8.2 nM. SB-699551 shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 can be used for the research of anxiety, breast cancer, and Alzheimer's disease [1] .
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1 Cited Publications
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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.
1
1 Cited Publications
Cat. No.: HY-B0391B
CAS No.: 1164469-60-6
Synonyms: KT-611 hydrochloride; BM-15275 hydrochloride
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Naftopidil hydrochloride (KT-611 hydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil hydrochloride has antiproliferative effects. Naftopidil hydrochloride can be used for the research of prostate hyperplasia [1].
Cat. No.: HY-B0702
CAS No.: 27848-84-6
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Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease [1] .
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ADRA1D receptor antagonist 1 is a potent, selective and orally active α1D adrenoceptor antagonist, with a Ki of 1.6 nM [1].
Cat. No.: HY-B0484
CAS No.: 35543-24-9
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Buflomedil hydrochloride, a vasodilator agent, is an orally active α1A-adrenoceptor antagonist with Kis of 4.06 µM and 6.84 µM for α1A-AR and α1B-AR, respectively. Buflomedil hydrochloride can be used for the study of peripheral circulatory disorders [1] .
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RS100329 hydrochloride is a potent and selective α1A-adrenoceptor antagonist with pKi values of 9.6, 7.9 and 7.5 for α1A, α1D, and α1B, respectively. RS100329 hydrochloride inhibits reflex urethral contractions. RS100329 hydrochloride can be used in research of benign prostatic hyperplasia [1] .
Cat. No.: HY-U00399A
CAS No.: 208992-74-9
Synonyms: ABT 980
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Fiduxosin hydrochloride (ABT 980) is a potent α1-adrenoceptor antagonist, with Ki of 0.160 nM, 24.9 nM, and 0.920 nM for α1a-, α1b-, and α1d-adrenoceptors, respectively [1].
Cat. No.: HY-B0371B
CAS No.: 109351-34-0
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(R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively [1].
Synonyms: SZL 49
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Prazobind (SZL 49), a prazosin analog, is an irreversible α1-adrenoceptor antagonist. Prazobind competes for alpha 1-adrenoceptor binding sites with a similar potency (IC50 of 1 nM) in tissues enriched in both the alpha 1A (hippocampus) and alpha 1B (liver) subtypes. Prazobind partially inhibits the contractions of circular muscles, longitudinal muscles and smooth muscles of the spleen. Prazobind can be used for the study of blood pressure [1] .
Cat. No.: HY-B0371D
CAS No.: 109351-33-9
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(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity α-adrenoceptor antagonist with Ki values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 729 nM, 3.5 nM and 46.4 nM, respectively [1].
Cat. No.: HY-U00237
CAS No.: 200050-59-5
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L-771688 is a highly selective α1A-Adrenoceptor antagonist with a Ki of 0.43±0.02 nM.
Cat. No.: HY-U00399
CAS No.: 208993-54-8
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Fiduxosin is a potent α1-adrenoceptor antagonist, with Ki of 0.160 nM, 24.9 nM, and 0.920 nM for α1a-, α1b-, and α1d-adrenoceptors, respectively.
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5-Methylurapidil isα1A‐adrenoceptor antagonist. 5-Methylurapidil can be used for the research of cardiovascular diseases such as hypertension and heart failure [1].
Cat. No.: HY-120296R
CAS No.: 34661-85-3
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5-Methylurapidil (Standard) is the analytical standard of 5-Methylurapidil. This product is intended for research and analytical applications. 5-Methylurapidil isα1A‐adrenoceptor antagonist. 5-Methylurapidil can be used for the research of cardiovascular diseases such as hypertension and heart failure [1].
Cat. No.: HY-U00333
CAS No.: 161905-64-2
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α1 adrenoceptor-MO-1, an S enantiomer, has affinity at alpha 1 adrenergic receptor, shows alphalytic activity, and possesses analgesic action; more active than R enantiomer.
Cat. No.: HY-129427
CAS No.: 149847-87-0
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DC-015 is a selective and orally active alpha 1-adrenoceptor antagonist on plasma lipid and vascular reactivity in hyperlipidaemic rodent model. DC-015 is a synthesized quinazoline derivative. DC-015 decreases mean arterial pressure in rats. DC-015 has antihypertensive activity [1].
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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
