TASP0434299
TASP0434299 (Compound 10) is a labeled 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.
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- CAS No.: 1520893-08-6
- Formule: C27H35N5O5
- Masse moléculaire:509.61
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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V1b Receptor |
TASP0434299 (60 min) potently inhibits the binding of [3H]AVP to cell membranes of 293FT cells expressing human V1B receptors, with an IC50 of 0.526 nM[2].
TASP0434299 (60 min) potently inhibits the binding of [3H]AVP to rat anterior pituitary membranes expressing endogenous rat V1B receptors, with an IC50 of 0.641 nM[2].
TASP0434299 (30 min) potently antagonizes AVP-induced [Ca2+]ᵢ elevation in Chinese hamster ovary K1 cells expressing human V1B receptors, with an IC50 of 0.639 nM[2].
TASP0434299 (1 μM) is a substrate of human P-glycoprotein, with an efflux ratio of 27.9 when detected at a concentration of 1 μM in LLC-GA5-COL300 cells[2].
TASP0434299 (1 μM; co-incubated with [3H]TASP0434299 for 120 min) completely blocks the specific binding of [3H]TASP0434299 to native rat V1B receptors in rat anterior pituitary slices[2].
TASP0434299 (1 μM; co-incubated with [3H]TASP0434299 for 120 min) completely blocks the specific binding of [3H]TASP0434299 to native rhesus monkey V1B receptors in rhesus monkey anterior pituitary slices[2].
TASP0434299 potently and selectively binds to human V1B Rs with an IC50 of 0.526 nM, and exhibits no detectable affinity for human V1A, V2 or oxytocin receptors[3].
TASP0434299 potently antagonizes human V1B R-mediated intracellular calcium mobilization, with an IC50 of 0.639 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
11C-TASP0434299 (0.01-10.7 mg/kg; intravenous injection; single administration) binds specifically to endogenous vasopressin V1B receptors in the pituitary gland of rhesus monkeys[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, weight 234.9-293.4 g)[2]
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Dosage:0.93 nM/kg ([3H]-labeled); 0.41, 0.80, 1.9, 4.2, 8.7 nmol/kg (unlabeled, co-administered)
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Administration:i.v.
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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.
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Animal Model:Macaca mulatta (male, 5.2-6.5 kg)[3]
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Dosage:406 MBq (radioactivity, range 361-467 MBq); 6.1 μg (mass dose, range 2.9-10 μg)
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Administration:i.v.
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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.
Chemical Information
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CAS No. 1520893-08-6
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Masse moléculaire 509.61
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Formule C27H35N5O5
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SMILES
O=C1C2=CC(OCCCN3CCOCC3)=CN=C2N=C(C=4C=CC=C(OC)C4)N1CC(=O)NC(C)(C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Kazumi Koga, et al. Radioactively labeled ligand of v1b receptor. JP2015120644A. 2018-08-22
[2]. Koga K, et al. TASP0434299: A Novel Pyridopyrimidin-4-One Derivative as a Radioligand for Vasopressin V1B Receptor. J Pharmacol Exp Ther. 2016;357(3):495-508. [Content Brief]
[3]. Koga K, et al. High-Contrast PET Imaging of Vasopressin V1B Receptors with a Novel Radioligand, 11C-TASP699. J Nucl Med. 2017;58(10):1652-1658. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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