57
3
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T74557 |
α1A-AR Degrader 9c
|
PROTACs | PROTAC |
α1A-AR Degrader 9c(化合物 9c)是一种高效、选择性且可逆的α1A-AR PROTAC降解剂,DC50值为2.86 μM。它通过蛋白酶体途径诱导α1A-AR的降解,并且在抑制PC-3细胞增殖方面表现出活性,IC50为6.12 μM。此外,α1A-AR Degrader 9c展现出在前列腺癌研究中的抗肿瘤潜力。 | |||
T41231 |
GP 1a
|
Cannabinoid Receptor; PERK; Arrestin | Apoptosis; GPCR/G Protein |
GP 1a 是cannabinoid receptor 2(CB2)的强效激动剂(EC50=7.1),是在cAMP、GTPγS 和β-arrestin 招募试验中显示的。GP 1a 对CB2受体的选择性约为CB1受体的30倍,且在体外增加HL-60细胞的P-ERK1/2表达。GP 1a 对皮肤伤口愈合有益。GP 1a 可抑制炎症和纤维生成,同时促进上皮的重新形成。 | |||
T1132 |
Nicergoline
尼麦角林,Nicergolinum,Nimergoline |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Nicergoline (Nicergolinum) 是一种有效的,选择性的、具有口服活性的α1A-肾上腺素能受体拮抗剂,是一种溴烟碱酸的麦角林衍生物。它具有血管舒张作用,可以改善阿尔茨海默症小鼠的认知功能。 | |||
T38160 |
STING Agonist 1a
|
||
STING agonist 1a is an agonist of stimulator of interferon genes (STING).1It induces expression of an IRF-inducible SEAP reporter gene in a cell-based assay (EC50= 16.77 μM). STING agonist 1a (12.5-100 μM) induces expression of IFN-β, IL-6, and chemokine (C-X-C motif) ligand 10 (CXCL10) in THP-1 cells, an effect that can be reversed by STING knockout or the STING inhibitor H-151 . 1.Hou, H., Yang, R., Liu, X., et al.Discovery of triazoloquinoxaline as novel STING agonists via structure-based vir... | |||
T76469 |
Esculentin 1A
|
||
Esculentin 1A 是一种青蛙皮肤来源的抗菌肽(AMP),具有强大的体外抗假单胞菌活性。 | |||
T30873 |
Chelator 1a
Chelator1a,Chelator-1a |
Antifungal | Microbiology/Virology |
Chelator 1a 具有抗真菌活性,抑制曲霉菌和念珠菌,可用于研究真菌感染和癌症。 | |||
T63873 | Anti-Aβ agent 1A | ||
Anti-Aβ agent 1A 是有效的抗淀粉样蛋白-β (amyloid-β) 剂。Anti-Aβ agent 1A 可明显抑制 LPS 诱导的 IL-1β、IL-6 和 TNF-α 水平,并能够利用线粒体途径减少 H2O2诱导的 SH-SY5Y 细胞凋亡,表现出抗氧化、抗炎、抗 Aβ 毒性和神经保护活性。Anti-Aβ agent 1A 能够用于研究阿尔兹海默症。 | |||
T83857 |
Soluble Epoxide Hydrolase PROTAC 1a
sEH Proteolysis-targeting Chimera 1a,Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a,sEH PROTAC 1a |
||
Soluble epoxide hydrolase (sEH) PROTAC 1a是一种利用蛋白质降解靶向嵌合体(PROTAC)技术,通过连接区域将cereblon配体1与sEH抑制剂t-TUCB结合。该化合物通过促进sEH的降解,特异性抑制sEH的水解酶活性(IC50 = 0.8 nM),相较于其磷酸酶活性(IC50 = >10,000 nM)具有较高选择性。sEH PROTAC 1a还特定促进细胞质中而非过氧体中的sEH降解,并通过溶酶体而非蛋白酶体实现其降解。它能够降低thapsigargin诱导的HepG2与293T细胞中磷酸化的inositol-requiring enzyme 1α (IRE1α)水平和X-box结合蛋白1 (XBP1)剪接,表明能减少ER应激。 | |||
T36045 |
1a,1b-dihomo Prostaglandin E2
1a,1b-dihomo Prostaglandin E2 |
||
1a,1b-dihomo Prostaglandin E2 (PGE2) is a rare polyunsaturated fatty acid first identified in extracts of sheep vesicular gland microsomes, known to contain COX, incubated with adrenic acid . 1a,1b-dihomo PGE2 has also been identified in conditioned media of RAW 264.7 macrophages stimulated with endotoxin and arachidonic acid . This product is thought to be produced by elongation of AA to adrenic acid, which is then metabolized sequentially by COX and PGE synthase. | |||
T36219 |
1a,1b-dihomo Prostaglandin E1
1a,1b-dihomo Prostaglandin E1 |
||
1a,1b-dihomo Prostaglandin E1 是一类前列腺素化合物。 | |||
T131451 |
Methyl 1a,7a,14a-triacetoxy-8,15-isopimaredien-18-oate
|
||
Methyl 1a,7a,14a-triacetoxy-8,15-isopimaredien-18-oate 是一种有用的有机化合物,可用于生命科学领域的相关研究,其产品编号为 T131451。 | |||
T16798 |
RS 17053 hydrochloride
RS-17053 |
Others; Adrenergic Receptor | GPCR/G Protein; Neuroscience; Others |
RS 17053 hydrochloride 是有效的、选择性的 α1A 肾上腺素受体 (α1A adrenoceptor) 拮抗剂。RS 17053 hydrochloride 在细胞膜中测得的 pKi 值为 9.1,功能分析的 pA2 值为 9.8。 | |||
T12643 |
(R)-Terazosin
(R)-特拉唑嗪,盐酸特拉唑嗪 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
(R)-Terazosin 是一种 Terazosin 的活性 R 型对映体, 是 α1-肾上腺素受体拮抗剂,对 α1a,α1b 和α1d-肾上腺素受体的Ki 分别为 6.51 nM,1.01 nM 和 1.97 nM。 | |||
T23301 |
(S)-(+)-Niguldipine hydrochloride
|
Others | Others |
(S)-(+)-Niguldipine hydrochloride is a L-type Ca2+ channel blocker and α1A-adrenoceptor antagonist. | |||
T23253 |
RS 100329 hydrochloride
RS-100329 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
RS 100329 hydrochloride 是α1A 肾上腺素能受体的拮抗剂。 | |||
T9762 |
Upidosin
SB-216469,SB 216469,Rec 15-2739,Recordati 15/2739 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Upidosin (SB-216469) 是一种有效的、选择性的α1-肾上腺素受体拮抗剂,α1a 亚型Ki=0.34nM,α1b 亚型Ki=3.9nM,β1d 亚型Ki=1.5nM,γ2-肾上腺素受体Ki=33.3nM。 | |||
T13110 |
Tedatioxetine hydrobromide
Lu AA 24530 hydrobromide |
Dopamine Receptor; 5-HT Receptor; Norepinephrine | GPCR/G Protein; Neuroscience |
Tedatioxetine hydrobromide (Lu AA 24530 hydrobromide) 是一种血清素-去甲肾上腺素-多巴胺再摄取抑制剂 ,也是 5-HT2A、5-HT2C、5-HT3 和 α1A-肾上腺素能受体的拮抗剂,可用于治疗抑郁症和焦虑症。 | |||
T15688 |
L-771688
SNAP 6383 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
L-771688(SNAP 6383) 是一种新型有效和选择性的 α1A-肾上腺素受体拮抗剂, Ki 值为 0.43±0.02 nM。L-771688 KE 用于治疗良性前列腺增生。 | |||
T9220 |
Naftopidil hydrochloride
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-,萘哌地尔盐酸盐,KT-611 hydrochloride,BM-15275 hydrochloride |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Naftopidil hydrochloride (BM-15275 hydrochloride) 是一种选择性的 alpha1-肾上腺素受体 (α1-adrenoceptor) 拮抗剂,对克隆的人类 α1a、α1b 和 α1d 亚型肾上腺素受体的亲和力 Ki 分别为 3.7 nM、20 nM、1.2 nM。它具有抗增殖活性,可用于研究前列腺增生。 | |||
T1504 |
Silodosin
西洛多辛,KAD 3213,KMD 3213 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Silodosin (KAD 3213) 是有选择性的、强效的、口服活性的 α1A-adrenergic receptor 阻滞剂,是一种有效且耐受性良好的试剂,可用于研究 LUTS/BPH。它对 α1A-AR 表现出高度的亲和力,是 α1B-AR 和 α1D-AR 亲和力的 162 和 50 倍。 | |||
T11286 |
Fiduxosin
A 185980.1,ABT 980 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Fiduxosin 是一种具有选择性和有效性的 α1-adrenoceptor 拮抗剂,对 α1a-adrenoceptor,α1b-adrenoceptor 和 α1d-adrenoceptor 有抑制作用,Ki 值分别为 0.160 nM,24.9 nM 和 0.920 nM。Fiduxosin 可用于治疗良性前列腺增生。 | |||
T1090 |
Perphenazine
Perphenazin,Etaperazine,Trilafon,奋乃静 |
CaMK; Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Perphenazine (Trilafon) 是吩噻嗪衍生物和多巴胺拮抗剂,具有止吐和抗精神病特性。它能够抑制5-HT2A 受体,α1A 肾上腺素能受体,多巴胺D2、D3、D2L 受体,以及组胺H1受体,对应的Ki 值分别为5.6、10、0.765、0.13、3.4 和 8 nM。 | |||
T6600 |
Naftopidil dihydrochloride
KT-611,KT-611 2HCl,盐酸萘哌地尔,Naftopidil DiHCl |
5-HT Receptor; Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Naftopidil dihydrochloride (KT-611 2HCl) 是一种选择性的 alpha1-肾上腺素受体 (α1-adrenoceptor) 拮抗剂,对克隆的人类 α1a、α1b 和 α1d 亚型肾上腺素受体的亲和力Ki 分别为 3.7 nM、20 nM、1.2 nM。它具有抗增殖活性,可用于研究前列腺增生。 | |||
T3046 |
BMY 7378 dihydrochloride
BMY7378 HCl |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor | GPCR/G Protein; Neuroscience |
BMY 7378 dihydrochloride (BMY7378 HCl) 是选择性 α1D 肾上腺素受体拮抗剂,也是5-HT1A 受体部分激动剂。它同表达克隆大鼠 α1D-AR 的膜结合的亲和力 (Ki=2 nM) 是同克隆大鼠 α1A-AR (Ki=800 nM) 或仓鼠 α1B-AR (Ki=600 nM) 结合的亲和力 的100 以上。 | |||
T27401 |
Garomefrine HCl
PNO-49B,NS-49,ABT-232,ABT232,NS49,PNO49B |
||
Garomefrine HCl, a α1A-adrenoceptor agonist, is potential for the treatment of urinary incontinence. | |||
T10523 |
β3-AR agonist 1
|
Others | Others |
β3-AR agonist 1 is a highly selective, and orally available agonist of β3-adrenergic receptor (EC50: 18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold). | |||
T80505 |
PKCα (C2-4) inhibitor peptide
|
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
PKCα(C2-4) inhibitor peptide为专一性PKCα抑制剂,能够抑制α1A‐肾上腺素受体激动剂A-61603对IKr通道的影响。 | |||
T14972 |
Cirazoline hydrochloride
LD 3098 hydrochloride |
Others | Others |
Cirazoline hydrochloride is a competitive full agonist of the α1A-adrenergic receptor (α1A-AR; Ki: 120 nM). It is a partial agonist at α1B-AR (Ki: 960 nM) and α1D-AR (Ki: 660 nM). | |||
T24378 |
L-771688 dihydrochloride
L 771688 dihydrochloride |
||
L-771688 is an α1A-adrenoceptor antagonist potentially for the treatment of benign prostatic hyperplasia. | |||
T82072 |
Indoramin hydrochloride
Indoramine hydrochloride,Wy 21901 hydrochloride |
||
Indoramin (hydrochloride) is a novel antihypertensive agent that exhibits selectivity for the α1A-adrenergic receptor. | |||
T23532 |
WB 4101 hydrochloride
|
Others | Others |
α1A-adrenergic antagonist | |||
T23374 |
SNAP 5089
|
Others | Others |
α1A-adrenoceptor antagonist | |||
T28617 |
RS 100329
RS100329 HCl,RS 100329 HCl,RS100329,RS-100329 |
||
RS 100329 HCl is a selective α1A-adrenoceptor antagonist (pKi = 9.6 for human cloned α1A receptors). | |||
T23225 |
(R)-(-)-Niguldipine hydrochloride
|
Others | Others |
(R)-(-)-Niguldipine hydrochloride is a L-type Ca2+ channel blocker and α1A-adrenoceptor antagonist. | |||
T71335 | PF-3774076 | ||
PF-3774076 is a CNS penetrant, potent, selective, partial agonist at the human α1A adrenoceptor. PF-3774076 is selective over α1B and α1D adrenoceptors. | |||
T80477 |
Muscarinic toxin 3
MT3 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Muscarinic toxin 3 (MT3) 是高效的非竞争性mAChR及adrenoceptors拮抗剂,对M1、M4、α1A、α1B、α1D、α2A、α2B、α2C受体展示出不同程度的选择性,其pIC50值分别为6.71、8.79、8.86、7.57、8.13、8.49、6.5、7.29。该化合物具有显著的肾上腺素受体抑制活性。 | |||
T12815 |
(S)-Terazosin
|
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity antagonist of α-adrenoceptor(α1a, α1b and α1d-adrenoceptor with Ki values of 3.91 nM, 0.79 nM and 1.16 nM, respectively). | |||
T35576 |
Phenylephrine-3-O-Sulfate
|
||
Phenylephrine-3-O-sulfate is metabolite of the α1A-adrenergic receptor agonist phenylephrine formed via sulfation. | |||
T36071 |
Silodosin Glucuronide (sodium salt)
|
||
Silodosin glucuronide is an active metabolite of the α1A-adrenergic receptor antagonist silodosin . It is formed from silodosin by the UDP-glucuronosyltransferase (UGT) isoform UGT2B7. Silodosin glucuronide is toxic to rats with an LD50 value of 0.347 mg/kg. | |||
TP2086 |
AdTx1
|
||
Selective, high affinity, non-competitive α1A adrenoceptor antagonist (Ki = 0.35 nM). Exhibits no significant activity against a range of other GPCRs, including α2A, β1 and β2 adrenoceptors. Antagonizes effects of phenylephrine on isolated rabbit prostate | |||
T63980 |
BODIPY FL prazosin
|
||
BODIPY FL prazosin 是荧光 α1-肾上腺素 α1-adrenergic 拮抗剂,能够作用于 α1a-AR (Ki: 14.5 nM)和 α1b-AR (Ki: 43.3 nM)。BODIPY FL prazosin 是一种荧光配体,激发和发射波长分别为 485 和 535 nm。BODIPY FL prazosin 能够用于 α1-肾上腺素受体亚型的亚细胞定位差异的研究。 | |||
T64314 |
OxyMetazoline
|
||
OxyMetazoline 是一种 α-肾上腺素受体 (α-adrenoceptor) 激动剂,能够作用于 α1A (IC50: 0.02 μM)、α1B (IC50: 0.25 μM)、α2A (IC50: 0.58 μM) 和 α2C (IC50: 0.13 μM)。OxyMetazoline 能够用于研究缓解鼻黏膜充血。 | |||
T80175 |
Conopeptide rho-TIA
|
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Conopeptide rho-TIA为从掠食性海螺Conus tulipa毒液中提炼的多肽,对人类α1B-Adrenergic Receptor呈现非竞争性抑制作用,同时对α1A-Adrenergic Receptor和α1D-Adrenergic Receptor表现出竞争性抑制。Conopeptide rho-TIA与这些亚型的结合特性可能对开发针对α1-Adrenergic Receptor亚型的选择性新药具有参考价值。 | |||
T5384 |
RS 504393
|
CCR | Immunology/Inflammation; Microbiology/Virology |
RS 504393 是一种高度选择性的 CCR2 趋化因子受体拮抗剂,作用于人重组 CCR2 和 CCR1 受体,IC50值分别为 89 nM 和大于 100 μM。 | |||
T69031 |
Cirazoline (free base)
|
||
Cirazoline (free base) is a full agonist at the α1A adrenergic receptor, a partial agonist at both the α1B and α1D adrenergic receptors, and a nonselective antagonist to the α₂ adrenergic receptor. It is believed that this combination of properties could make cirazoline an effective vasoconstricting agent. | |||
TQ0283 |
RS102895
|
CCR | Immunology/Inflammation; Microbiology/Virology |
RS102895 是一种CCR2拮抗剂,IC50值为 360 nM。 | |||
T78626 |
LY393615
NCC1048 |
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
LY393615 (NCC1048) 是新型神经元 Ca2+ 与 Na+ 通道阻断剂,具备优良的脑渗透性,并在脑缺血模型中显示神经保护效果,适用于神经性疾病研究。 | |||
T67694 |
ZY-19489
|
Parasite | Microbiology/Virology |
ZY-19489是一种具有抗疟作用的化合物, 是一种潜在的单剂量根治性恶性疟原虫和间日疟原虫疟疾的药物,已获得美国 FDA 的孤儿药认定。 | |||
T37794 | Rec 15/2615 (hydrochloride) | ||
Rec 15/2615 is an antagonist of α1B-adrenergic receptors (α1B-ARs; Ki = 0.45 nM for the recombinant human receptor).1 It selectively inhibits α1B-ARs over α1A-, α1D-, and α1L-ARs (Kis = 7.59, 10.23, and 49 nM, respectively). Rec 15/2615 inhibits norepinephrine-induced contractions of isolated rabbit prostate and urethral strips (Kis = 100 and 316.2 nM, respectively), as well as reduces norepinephrine-induced contractions of chloroethylclonidine-precontracted isolated rabbit aortic rings (Ki = 50... | |||
T0696 |
Naftopidil
KT-611,萘哌地尔,BM-15275 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Naftopidil (KT-611) 是一种选择性的 alpha1-肾上腺素受体 (α1-adrenoceptor) 拮抗剂,对克隆的人类 α1a、α1b 和 α1d 亚型肾上腺素受体的亲和力Ki 分别为 3.7 nM、20 nM 、1.2 nM。它具有抗增殖活性,可用于研究前列腺增生。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN4117 | GB 1a | Antioxidant; Tyrosinase | oxidation-reduction; Proteases/Proteasome |
GB 1a 是一种从藤黄 Garcinia travancorica 叶中分离出来的天然产物。 | |||
T17310 |
Phenylephrine
去氧肾上腺素,L-Phenylephrine,去氧肾上腺素碱,(R)-(-)-Phenylephrine |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Phenylephrine ((R)-(-)-Phenylephrine) 是一种选择性的α1-肾上腺素受体激动剂,常用作减充血剂。 | |||
T0453 |
Phenylephrine hydrochloride
NCI-c55641,Phenylephrine HCl,盐酸去氧肾上腺素,(R)-(-)-Phenylephrine hydrochloride |
Endogenous Metabolite; Adrenergic Receptor | GPCR/G Protein; Metabolism; Neuroscience |
Phenylephrine hydrochloride (NCI-c55641) 是选择性的α1-肾上腺素能受体激动剂,对α1A,α1B 和α1D 受体的pKis 分为4.70,4.87和5.86。 |