Search Result
Results for "
α1D
" in MedChemExpress (MCE) Product Catalog:
7
Isotope-Labeled Compounds
| Cat. No. |
상품명 |
Target |
연구분야 |
Chemical Structure |
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- HY-B0471
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-
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- HY-10122
-
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KAD 3213; KMD 3213
|
Adrenergic Receptor
Bacterial
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Endocrinology
Cancer
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Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH [1] .
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- HY-N1255
-
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(-)-Scoulerine; Discretamine
|
Bcl-2 Family
Apoptosis
mTOR
GABA Receptor
PI3K
Adrenergic Receptor
Beta-secretase
Akt
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Cancer
|
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Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine mainly targets the PI3K/Akt/mTOR signaling axis and α1D-adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine is applicable to research related to leukemia, ovarian cancer, and colorectal cancer [1] .
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- HY-100554
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Adrenergic Receptor
5-HT Receptor
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Cardiovascular Disease
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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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- HY-101300
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LD 3098 hydrochloride
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Adenosine Receptor
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Neurological Disease
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Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full α1A-adrenergic receptor (α1A-AR) agonist (Ki=120 nM) and only a partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR (Ki=660 nM) [1].
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- HY-B0391
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KT-611; BM-15275
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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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] .
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- HY-135270
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-
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- HY-U00399A
-
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ABT 980
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Adrenergic Receptor
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Endocrinology
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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].
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- HY-B0471R
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(R)-(-)-Phenylephrine hydrochloride (Standard); L-Phenylephrine hydrochloride (Standard)
|
Reference Standards
Adrenergic Receptor
Endogenous Metabolite
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Cardiovascular Disease
Endocrinology
Cancer
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Phenylephrine (hydrochloride) (Standard) is the analytical standard of Phenylephrine (hydrochloride). This product is intended for research and analytical applications. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
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- HY-B0371B
-
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Adrenergic Receptor
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Endocrinology
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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].
|
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- HY-103204
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Adrenergic Receptor
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Endocrinology
|
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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] .
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- HY-12697
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Dopamine Receptor
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Neurological Disease
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NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis [1] .
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- HY-B0371D
-
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Adrenergic Receptor
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Endocrinology
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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].
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- HY-U00399
-
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Adrenergic Receptor
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Endocrinology
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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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- HY-19268
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GW 1818
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Adrenergic Receptor
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Metabolic Disease
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GG-818 (GW 1818) is a potent and selective α1 adrenoceptor antagonist, with pKi values of 9.7 for α1a, 7.8 for α1b, and 7.6 for α1d. GG-818 (GW 1818) can be used for benign prostatic hyperplasia research [1].
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- HY-120473
-
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Adrenergic Receptor
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Metabolic Disease
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TAK-259 is an orally active α1D-adrenergic receptor antagonist with a Ki value of 1.1 nM for human α1D-adrenergic receptors. TAK-259 can inhibit the contraction of isolated bladder strips in rats with bladder outlet obstruction, reduce non-voiding bladder contractions, and improve urinary frequency symptoms. TAK-259 can be used in research related to overactive bladder [1].
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- HY-116623
-
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Adrenergic Receptor
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Endocrinology
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A-123189 is a selective and potent α1D antagonist with Kis of 0.312 and 0.17 for human α1D and rat α1D, respectively. A-123189 displays selectivities between 10- to 20-fold for the α1D receptor over the human α1A and rat α1A receptors [1].
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- HY-B0471S
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(R)-(-)-Phenylephrine-d3 hydrochloride; L-Phenylephrine-d3 hydrochloride
|
Adrenergic Receptor
Endogenous Metabolite
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Cardiovascular Disease
Endocrinology
|
|
Phenylephrine-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
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- HY-125641
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5-HT Receptor
Adrenergic Receptor
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Cardiovascular Disease
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AL-34662 is a selective 5-HT2A receptoragonist (IC50: 0.77 nM and 1.5 nM for rat and human 5-HT2 receptor). AL-34662 is also a weak α-1D adrenergic agonist activity (EC50:0.4 μM). AL-34662 is an ocular hypotensive agent [1] .
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- HY-B0471S1
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(R)-(-)-Phenylephrine-2,4,6-d3 hydrochloride; L-Phenylephrine-2,4,6-d3 hydrochloride
|
Adrenergic Receptor
Endogenous Metabolite
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Cardiovascular Disease
Endocrinology
|
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Phenylephrine-2,4,6-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
|
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- HY-103209
-
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
|
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Rec 15/2615 hydrochloride is a potent and selective α-1B adrenoceptor antagonist with Ki values of 1.9 nM, 0.3 nM, 2.6 nM for α1A, α1B, α1D, respectively. Rec 15/2615 hydrochloride modulates vaginal smooth muscle contractility and genital engorgement [1] .
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- HY-113918
-
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PTHR
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Metabolic Disease
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SW-106 is a selective antagonist of parathyroid hormone/parathyroid hormone-related peptide receptor (PPR) and PTHR1, with an IC50 value of 0.99 μM against PPR. SW-106 antagonizes cAMP responses. SW-106 can be used in the research of osteoporosis [1] .
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- HY-B0391A
-
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KT-611 dihydrochloride; BM-15275 dihydrochloride
|
Adrenergic Receptor
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Cancer
|
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Naftopidil dihydrochloride (KT-611 dihydrochloride) 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 dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia [1] .
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- HY-123514
-
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Adrenergic Receptor
Dopamine Receptor
5-HT Receptor
|
Others
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SNAP8719 free base is a selective α1D-adrenoceptor antagonist (pKi = 8.89). SNAP8719 free base shows affinity for the dopamine D2-, 5-HT1A-, and the human clonal α2a-adrenoceptor, with pKi values of 5.98, 6.47, and <5.0, respectively. SNAP8719 free base causes a concentration-dependent increase in the twitch response [1].
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- HY-175669
-
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Chloride Channel
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Metabolic Disease
Endocrinology
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ANO1-IN-5 is an orally active ANO1 inhibitor with an IC50 of 4.57 μM. J ANO1-IN-5 demonstrates 118-, 642-, and 10000-fold selectivity over α1A-,α1B-, andα1D-AR, respectively. ANO1-IN-5 exhibits significant inhibitory effects on osteoclast differentiation and function. ANO1-IN-5 can used for the study of osteoporosis [1].
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- HY-P5158
-
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Adrenergic Receptor
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Others
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Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs [1].
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- HY-116982
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Adrenergic Receptor
5-HT Receptor
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BMY 7378 (free base) is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 (free base) 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 (free base) is a 5-HT1A receptor partial agonist [1] .
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- HY-W724254
-
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Adrenergic Receptor
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Endocrinology
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SNAP-6201 is a selective α1a adrenoceptor antagonist with a Ki of 0.2 nM. SNAP-6201 exhibits >1400-fold selectivity over α1b and α1d adrenoceptors. SNAP-6201 exhibits excellent selectively to inhibit intraurethral pressure (IUP) in the anesthetized dog model. SNAP-6201 can be used for benign prostatic hyperplasia (BPH) research [1].
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- HY-148252
-
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Adrenergic Receptor
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Endocrinology
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ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.
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- HY-119262
-
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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ABT-866 is an α1A-adrenoceptor agonist and an antagonist at the α1B- and α1D-adrenoceptor subtypes. ABT-866 has an EC50 of 0.60 μM for the α1A in the rabbit urethra. ABT-866 has a pA2 value of 5.4 for the α1B in the rat spleen. ABT-866 has a pA2 value of 6.2 for the α1D 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 [1] .
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- HY-B0471S3
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- HY-B0471S2
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- HY-135488
-
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Adrenergic Receptor
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Cardiovascular Disease
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A 131701 is a selective α1a- (Ki: 0.22 nM for human α1a) and α1d-adrenoceptor antagonist. A 131701 antagonizes epinephrine-induced increases in intraurethral pressure (IUP). A 131701 causes transient decreases in mean arterial blood pressure (MABP) and transient tachycardia. A 131701 can be used in the research of spontaneous hypertension [1].
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- HY-B0391B
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KT-611 hydrochloride; BM-15275 hydrochloride
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Adrenergic Receptor
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Cancer
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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].
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- HY-B0391S1
-
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KT-611-d5; BM-15275-d5
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Isotope-Labeled Compounds
Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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Naftopidil-d5 is deuterium labeled Naftopidil. 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] .
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- HY-101300R
-
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LD 3098 hydrochloride (Standard)
|
Reference Standards
Adenosine Receptor
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Neurological Disease
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|
Cirazoline (hydrochloride) (Standard) is the analytical standard of Cirazoline (hydrochloride). This product is intended for research and analytical applications. Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full?α1A-adrenergic receptor (α1A-AR) agonist (Ki=120 nM) and only a partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR (Ki=660 nM) [1].
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- HY-B0391R
-
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KT-611 (Standard); BM-15275 (Standard)
|
Reference Standards
Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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|
Naftopidil (Standard) is the analytical standard of Naftopidil. This product is intended for research and analytical applications. 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] .
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- HY-B0391S2
-
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KT-611-d7; BM-15275-d7
|
Isotope-Labeled Compounds
Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
|
|
Naftopidil-d7 (KT-611-d7 ) is deuterium labeled Naftopidil. 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] .
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- HY-P5846
-
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MT3
|
mAChR
Adrenergic Receptor
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Neurological Disease
|
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Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity [1].
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- HY-162677
-
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Adrenergic Receptor
5-HT Receptor
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Cardiovascular Disease
|
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MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research [1].
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- HY-U00237B
-
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Adrenergic Receptor
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Others
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L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models [1].
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- HY-10122S
-
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Isotope-Labeled Compounds
Adrenergic Receptor
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Endocrinology
Cancer
|
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Silodosin-d4 is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH [1] .
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- HY-10122R
-
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KAD 3213 (Standard); KMD 3213 (Standard)
|
Reference Standards
Adrenergic Receptor
Bacterial
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Endocrinology
Cancer
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|
Silodosin (Standard) is the analytical standard of Silodosin. This product is intended for research and analytical applications. Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH [1] .
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- HY-100554R
-
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Adrenergic Receptor
Reference Standards
5-HT Receptor
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Cardiovascular Disease
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BMY 7378 (Standard) is the analytical standard of BMY 7378 (HY-100554). This product is intended for research and analytical applications. 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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- HY-120473A
-
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Adrenergic Receptor
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Metabolic Disease
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TAK-259 hydrochloride is an orally active α1D-adrenergic receptor antagonist with a Ki value of 1.1 nM for human α1D-adrenergic receptors. TAK-259 hydrochloride can inhibit the contraction of isolated bladder strips in rats with bladder outlet obstruction, reduce non-voiding bladder contractions, and improve urinary frequency symptoms. TAK-259 hydrochloride can be used in research related to overactive bladder [1].
|
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- HY-12697A
-
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Dopamine Receptor
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Neurological Disease
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NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 hydrochloride antagonizes Quinpirole-stimulated mitogenesis [1] .
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- HY-130418
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Adrenergic Receptor
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Cancer
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(-)-Domesticine is an anti-α-1D-adrenoceptor compound with cytotoxic activity. (-)-Domesticine showed activity in MTS cytotoxicity assays against human colon cancer cell lines HCT-116 and Caco-2. (-)-Domesticine tolerates alkoxy substituents and benzoate functional groups at the C1 position in modifications of its chemical structure. The most potent compounds of (-)-Domesticine have IC50 values in the range of 23-38 μM, similar to the known cytotoxic compound etoposide [1].
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- HY-103204R
-
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Reference Standards
Adrenergic Receptor
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Endocrinology
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RS100329 hydrochloride (Standard) is the analytical standard of RS100329 hydrochloride (HY-103204). This product is intended for research and analytical applications. 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] .
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- HY-183177
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Adrenergic Receptor
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Cardiovascular Disease
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Zolertine is an α-adrenergic receptor antagonist, with a pKi of 6.35 for rabbit α1A-adrenergic receptor and a pKi of 6.81 for rat α1B-adrenergic receptor. Zolertine competitively blocks α1D-adrenergic receptor-mediated vasoconstriction and α1A-adrenergic receptor-mediated vasoconstriction in arteries. Zolertine can be used in the research of hypertension [1].
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- HY-N1255A
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(-)-Scoulerine hydrochloride; Discretamine hydrochloride
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Apoptosis
PI3K
Akt
mTOR
Adrenergic Receptor
GABA Receptor
Beta-secretase
Bcl-2 Family
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Cancer
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Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine hydrochloride mainly targets the PI3K/Akt/mTOR signaling axis and α1D-adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine hydrochloride effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine hydrochloride also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine hydrochloride is applicable to research related to leukemia, ovarian cancer, and colorectal cancer [1] .
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- HY-183179
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Adrenergic Receptor
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Endocrinology
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α1A Adrenoceptor antagonist-1 is a selective α1A adrenoceptor antagonist with a human Ki <20 nM. α1A Adrenoceptor antagonist-1 exhibits activity against benign prostatic hyperplasia (BPH) to enable less hindered urine flow. α1A Adrenoceptor antagonist-1 relaxes α1a receptor-enriched urethral smooth muscle tissue without inducing hypotension. α1A Adrenoceptor antagonist-1 can be used for the research of benign prostatic hyperplasia (BPH) [1].
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- HY-118260
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Adrenergic Receptor
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Endocrinology
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Phendioxan is a compound with binding activity at the α(1)-adrenaline receptor subtype. The facilitated membrane diffusion of phendioxan is thought to be associated with improved α(1d)-AR affinity. Docking simulations of phendioxan at biological targets supported the stoichiometric analysis and revealed the importance of polar, electrostatic, hydrophobic, and shape effects of its phenoxy terminal orthogonal substituents on ligand binding [1].
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| Cat. No. |
상품명 |
Target |
Research Area |
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- HY-P5158
-
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Adrenergic Receptor
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Others
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Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs [1].
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- HY-P5846
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MT3
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mAChR
Adrenergic Receptor
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Neurological Disease
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Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity [1].
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| Cat. No. |
상품명 |
Category |
Target |
Chemical Structure |
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- HY-B0471
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- HY-N1255
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(-)-Scoulerine; Discretamine
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Alkaloids
Structural Classification
other families
Classification of Application Fields
Phenols
Polyphenols
Plants
Isoquinoline Alkaloids
Disease Research Fields
Source Classification
Cancer
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Bcl-2 Family
Apoptosis
mTOR
GABA Receptor
PI3K
Adrenergic Receptor
Beta-secretase
Akt
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Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine mainly targets the PI3K/Akt/mTOR signaling axis and α1D-adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine is applicable to research related to leukemia, ovarian cancer, and colorectal cancer [1] .
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- HY-B0471R
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- HY-N1255A
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(-)-Scoulerine hydrochloride; Discretamine hydrochloride
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Structural Classification
Alkaloids
Phenols
Polyphenols
Umbelliferae
Plants
Isoquinoline Alkaloids
Carphephorus corymbosus (Nutt.) Torr. & A.Gray
Source Classification
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Apoptosis
PI3K
Akt
mTOR
Adrenergic Receptor
GABA Receptor
Beta-secretase
Bcl-2 Family
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Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine hydrochloride mainly targets the PI3K/Akt/mTOR signaling axis and α1D-adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine hydrochloride effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine hydrochloride also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine hydrochloride is applicable to research related to leukemia, ovarian cancer, and colorectal cancer [1] .
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| Cat. No. |
상품명 |
Chemical Structure |
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- HY-B0471S
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Phenylephrine-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
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- HY-B0471S1
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Phenylephrine-2,4,6-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
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- HY-B0471S3
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Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
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- HY-B0471S2
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(S)-Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
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- HY-B0391S1
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Naftopidil-d5 is deuterium labeled Naftopidil. 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] .
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- HY-B0391S2
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Naftopidil-d7 (KT-611-d7 ) is deuterium labeled Naftopidil. 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] .
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- HY-10122S
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Silodosin-d4 is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH [1] .
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