2. GPCR/G Protein Membrane Transporter/Ion Channel
  3. Vasopressin Receptor P-glycoprotein
  4. TASP0434299

TASP0434299 (Compound 10) 是一种血管加压素 V1b 受体的放射性标记配体。TASP0434299 对人源和鼠源 V1B 受体表现出高结合亲和力，IC50 分别为 0.526 nM 和 0.641 nM，其对人源 V1B 受体具有强效拮抗活性，IC50 为 0.639 nM。TASP0434299 是人源和恒河猴 P-糖蛋白 (P-glycoprotein) 的底物，导致恒河猴脑摄取量较低。TASP0434299 可在体外和体内以饱和且特异性的方式与大鼠和猴垂体组织中的 V1B 受体结合。TASP0434299 经氚或 11C 放射性标记后，可作为原型 V1B receptor 放射性配体，通过正电子发射断层扫描技术实现麻醉猴垂体 V1B receptor 的可视化。

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TASP0434299

TASP0434299 Chemical Structure

CAS No. : 1520893-08-6

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TASP0434299 相关抗体

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V1a Receptor  V1b Receptor  V2 Receptor 

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TASP0434299 (Compound 10) is a radiolabeled ligand for the vasopressin V1b receptor. TASP0434299 exhibits high binding affinity for human and murine V1B receptors, with IC50 values of 0.526 nM and 0.641 nM, respectively, and shows potent antagonistic activity against the human V1B receptor with an IC50 of 0.639 nM. TASP0434299 is a substrate for human and rhesus monkey P-glycoprotein, resulting in low brain uptake in rhesus monkeys. TASP0434299 binds to V1B receptors in rat and monkey pituitary tissues in a saturable and specific manner both in vitro and in vivo. When radiolabeled with tritium or 11C, TASP0434299 serves as a prototype V1B receptor radiotracer to visualize V1B receptor in the pituitary gland of anesthetized monkeys via positron emission tomography[1][2][3].

IC50 & Target[1]

V1b Receptor 

 

体外研究
(In Vitro)

TASP0434299 (60 min) 可强效抑制[3H]AVP 与表达人 V1B 受体的 293FT 细胞膜的结合，其 IC50 为 0.526 nM[2]。
TASP0434299 (60 分钟) 可强效抑制[3H]AVP 与表达内源性大鼠 V1B 受体的大鼠垂体前叶膜的结合，其 IC50 为 0.641 nM[2]。
TASP0434299 (30 min) 可强效拮抗表达人 V1B 受体的中国仓鼠卵巢 K1 细胞中由 AVP 诱导的[Ca2+]ᵢ升高，其 IC50 为 0.639 nM[2]。
TASP0434299 (1 μM) 是人类 P-糖蛋白的底物，在 LLC-GA5-COL300 细胞中以 1 μM 浓度检测时，其外排率为 27.9[2]。
TASP0434299 (1 μM; 120 min co-incubated with [3H]TASP0434299) 可完全阻断特异性[3H]TASP0434299 与大鼠垂体前叶切片中天然大鼠 V1B 受体的结合[2]。
TASP0434299 (1 μM; 120 min co-incubated with [3H]TASP0434299) 可完全阻断 [3H]TASP0434299 对猕猴垂体前叶切片中天然恒河猴 V1B 受体的特异性结合[2]。
TASP0434299 可强效且选择性地结合人源 V1B Rs，其 IC50 为 0.526 nM，对人源 V1A、V2 或催产素受体无可检测的亲和力[3]。
TASP0434299 可强效拮抗人源 V1B R 介导的细胞内钙动员，其 IC50 为 0.639 nM[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

TASP0434299 相关抗体:
体内研究
(In Vivo)

[3H]TASP0434299 (0.93 nmol/kg；静脉注射；单次) 可与大鼠垂体前叶中的 V1B 受体产生特异性、可饱和的结合[2]。
11C-TASP0434299 (6.1 μg；静脉注射；单次) 可特异性结合恒河猴垂体中的内源性血管升压素 V1B 受体[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, weight 234.9-293.4 g)[2]
Dosage: 0.93 nmol/kg ([3H]-labeled); 0.41, 0.80, 1.9, 4.2, 8.7 nmol/kg (unlabeled, co-administered)
Administration: i.v.
Result: Detected specific membrane-bound radioactivity in the anterior pituitary, peaking at 30 minutes post-injection and gradually declining over 90 minutes.
Observed negligible radioactivity in the eye and cerebellum.
Demonstrated saturable membrane-bound radioactivity in the anterior pituitary, with an estimated B_max value of 18,300 dpm/mg protein (corresponding to 96 fmol/mg protein), matching in vitro B_max values for the rat V1B receptor.
Animal Model: Macaca mulatta (male, 5.2-6.5 kg)[3]
Dosage: 406 MBq (radioactivity, range 361-467 MBq); 6.1 μg (mass dose, range 2.9-10 μg)
Administration: i.v.
Result: Reached an approximate pituitary SUV of 2.0 at 90 minutes after injection.
Achieved an equilibrium specific-to-nondisplaceable uptake ratio of approximately 1.6.
Showed much lower radioactivity uptake and retention in temporal muscle compared to pituitary.
Exhibited almost negligible radioactivity in the brain.
分子量

509.61

Formula

C27H35N5O5
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

TASP0434299 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TASP04342991520893-08-6TASP 0434299TASP-0434299Vasopressin ReceptorP-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243GPCRsanterior pituitary receptorsratoxytocin receptorsarginine vasopressin V1B receptorChinese hamster ovary K1 cellshuman293FT cellsrhesus monkeyInhibitorinhibitorinhibit

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