Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T23513 |
VU10010
VU 10010 |
AChR | Neuroscience |
VU10010 (VU 10010) 是一种高度选择性的M4mAChR 变构增强剂,EC50为 400 nM。它与 M4mAChR 的变构位点结合,增强与 G 蛋白偶联,增加对乙酰胆碱的亲和力,还会增加卡巴胆碱引起的兴奋性传导抑制。 | |||
T23310 |
SB-203186 hydrochloride
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
SB 203186 hydrochloride 是一种选择性的、竞争性的5-HT4拮抗剂。它拮抗5-HT4受体介导的多巴酚收缩大鼠离体食管弛缓,其在大鼠食管、豚鼠回肠和人类结肠的 pKB 值分别是 10.9、9.5 和 9.0。 | |||
TP2209L |
Xenin 8 acetate
Xenin 8 acetate (117442-28-1 Free base) |
IGF-1R | Tyrosine Kinase/Adaptors |
Xenin 8 acetate 是神经降压素/异视素家族中 Xenin 的生物活性片段。 Xenin 8 acetate 增强精氨酸诱导的胰岛素释放(40%)并增强胰高血糖素对精氨酸(60%)和卡巴胆碱(50%)的反应。 | |||
T16686 |
Pyr10
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
Pyr10 是吡唑衍生物,是TRPC3通道的选择性抑制剂。Pyr10抑制卡巴可刺激的TRPC3转染的 HEK293 细胞中的 Ca2+流入。它具有区分受体操纵的TRPC3和天然基质相互作用分子 1 (STIM1)/Orai1 通道的能力。 | |||
T67956L |
Litoxetine HCl
litoxetine HCL(86811-09-8 Free base) |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Litoxetine HCl 是一种选择性5-羟色胺(5-HT)再摄取抑制剂(SSRI)和混合5-羟色胺拮抗剂,可用于治疗尿失禁。Litoxetine HCl 在没有抗毒蕈碱特性的浓度下(10 nM-1 microM)引起大鼠离体食道肌肉粘膜的浓度依赖性松弛,使卡巴胆碱张力降低达37%,更高浓度的Litoxetine HCl(3微摩-300微摩)与明显的松弛有关,直至取消卡巴胆碱张力。以前在离体豚鼠肠道中证明的利托西汀的抗心律失常活性,在浓度大于1 microM 时在大鼠离体食道肌肉粘膜中发挥了作用。 Litoxetine HCl 的5-HT 释放作用可以解释利托西汀对未处理的大鼠组织中的5-HT 诱导的松弛的效力,这种效力被pCPA 处理所逆转。 | |||
T67959 |
Pirodomast
|
Thrombin; Serine Protease | Proteases/Proteasome |
Pirodomast 是血栓素 A(TXA2)合成酶抑制剂。Pirodomast 能抑制白三烯(LT)D4、C4、E4 的形成和血栓素 B2(TXB2)的活性,但对组胺、甲氧胆碱、血清素、LTC4 或血小板活化因子诱导的豚鼠支气管痉挛的拮抗作用较弱或无效。Pirodomast 在体外对豚鼠气管只有微弱的松弛活性。Pirodomast 是一种潜在的抗过敏化合物,在体外可抑制胰蛋白酶的蛋白水解活性,在体内可阻止抗原诱发过敏绵羊的即时和晚期哮喘反应,抑制抗原诱导的过敏绵羊对组胺和卡巴胆碱的气道高反应性。 | |||
T34958 |
TRK-380
TAC301,TAC 301,TAC-301,TRK 380,TRK380 |
||
TRK-380 (TAC-301) is an effective and selective β3-adrenergic receptor agonist. TRK-380 improves formalin-induced frequent urination in rats and carbachol-induced bladder contraction in dogs (a decrease of 37.6%). | |||
T61529 |
Pirmenol hydrochloride
|
||
Pirmenol hydrochloride 通过阻断毒蕈碱性受体来抑制IK.ACh。Pirmenol 抑制 Carbachol 诱导的 IK.ACh,IC50值为 0.1 μM。 | |||
T61309 |
(R)-Oxybutynin
|
||
(R)-Oxybutynin (Aroxybutynin) is an orally active muscarinic receptor antagonist, which exhibits antimuscarinic, antispasmodic, and anticholinergic activity. This compound, being the (R)-isomer of Oxybutynin, competitively antagonizes Carbachol-induced contractions. It is particularly useful in researching neurogenic bladder dysfunction-related incontinence [1] [2] [3]. | |||
T37718 |
Galanin (rat, mouse) (trifluoroacetate salt)
GAL (rat, mouse),Galanin (rat, mouse) (trifluoroacetate salt) |
||
Galanin is a neuropeptide with diverse biological activities. [1][2][3][4][5] It binds to rat galanin (GAL) receptor subtypes GAL1-3 (IC50s = 0.339, 1.35, and 3.31 nM, respectively) and human GAL1-3 (IC50s = 0.288, 1.62, and 12.3 nM, respectively). [1] Galanin binds to and inhibits contraction of guinea pig gastric smooth muscle cells induced by carbachol . [2] In vivo, Galanin (6 nmol, i.c.v.) increases feeding behavior in rats and increases latency to hindpaw withdrawal in response to heat and... | |||
T83697 |
PAMP-12 (human, mouse, rat, porcine, bovine) TFA
Proadrenomedullin N-terminal 12 Peptide,PAMP (9-20) |
||
Proadrenomedullin N-terminal 12 peptide (PAMP-12) 是一种内源性肽段,源自人体肾上腺髓质,对应人类PAMP-20的9-20氨基酸,涉及降低血压。它是MAS相关G蛋白偶联受体家族成员X2 (MRGPRX2) 的激动剂。在表达人MRGPRX2的CHO细胞中,PAMP-12抑制forskolin诱导的cAMP积累(EC50 = 57.2 nM),特异性诱导表达MRGPRX2的CHO细胞的钙离子动员(EC50 = 41 nM),而在表达MRGPRX1、MRGPRX3或MRGPRX4的细胞中则无此效应(在1 µM浓度下)。PAMP-12还能作为烟碱型乙酰胆碱受体(nAChRs)的拮抗剂,抑制carbachol诱导的儿茶酚胺释放(IC50 = 1.3 µM)及钙和钠的流入(IC50分别为0.39 µM和0.87 µM),但不抑制组胺诱导的儿茶酚胺释放或钙和钠的流入(IC50 >1 µM),在初级牛肾上腺嗜铬细胞中有此表现。当以10至50 nmol/kg剂量给予正常血压大鼠时,PAMP-12能降低平均动脉血压。 |