SB-616234-A

Cat. No.: HY-19477 Purity: 98.14%: FAQs
Data Sheet SDS COA Handling Instructions

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SB-616234-A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.

For research use only. We do not sell to patients.

SB-616234-A Chemical Structure

CAS No. : 908601-49-0

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 682	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 682	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 780	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1180	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1600	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2200	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Protocol
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Description

SB-616234-A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.

In Vitro

SB-616234-A possesses high affinity for human 5-HT1B receptors stably expressed in Chinese hamster ovary (CHO) cells (pK_i 8.3 ± 0.2), and is over 100-fold selective for a range of molecular targets except h5-HT1D receptors (pK_i 6.6 ± 0.1). Similarly, affinity (pK_i) for rat and guinea pig striatal 5-HT1B receptors is 9.2 ± 0.1. In [³⁵S]-GTPγS binding studies in the human recombinant cell line, SB-616234-A acts as a high affinity antagonist with a pA₂ value of 8.6 ± 0.2 whilst providing no evidence of agonist activity in this system. In [³⁵S]-GTPγS binding studies in rat striatal membranes, SB-616234-A acts as a high affinity antagonist with an apparent pK_B of 8.4 ± 0.5, again whilst providing no evidence of agonist activity in this system. SB-616234-A (1 μM) potentiates electrically stimulated [³H]-5-HT release from guinea pig and rat cortical slices (S2/S1 ratios of 1.8 and 1.6, respectively)^[2].

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

In Vivo

SB-616234-A reverses the 5-HT1/7 receptor agonist, SKF-99101H-induced hypothermia in guinea pigs in a dose related manner with an ED₅₀ of 2.4 mg/kg p.o. SB-616234-A produces dose-related anxiolytic effects in both rat and guinea pig maternal separation-induced vocalisation models with an ED₅₀ of 1.0 and 3.3 mg/kg i.p., respectively^[1]. SB-616234-A (0.3-30 mg/kg p.o.) causes a dose-dependent inhibition of ex vivo [³H]-GR125743 binding to rat striatal 5-HT1B receptors with an ED₅₀ of 2.83 ± 0.39 mg/kg p.o^[1].

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

Molecular Weight

574.11

Formula

C₃₂H₃₆ClN₅O₃

CAS No.

908601-49-0

Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCC2=C1C=C(N3C[C@@H](C)N[C@@H](C)C3)C(OC)=C2)C4=CC=C(C5=CC=C(C6=NOC(C)=N6)C=C5C)C=C4.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (17.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7418 mL	8.7091 mL	17.4183 mL
5 mM	0.3484 mL	1.7418 mL	3.4837 mL
10 mM	0.1742 mL	0.8709 mL	1.7418 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.14%

Select Batch:

Data Sheet (282 KB) SDS (251 KB)

COA (259 KB) HNMR (205 KB) LCMS (110 KB)

Handling Instructions (2659 KB)

Animal Administration
^[1]

Seven days post surgery animals are placed in microdialysis cages for overnight habituation prior to microdialysis experimentation. The following morning microdialysis probes (2 mm cuprophane membrane) are implanted, via the guide cannulae, into the frontal cortex and/or dentate gyrus. Probes are perfused with artificial cerebrospinal fluid (aCSF) containing NaCl 145 mM, KCl 2.7 mM, MgCl₂ 1.0 mM, CaCl₂ 1.2 mM, Na₂HPO₄ 2.0 mM (pH 7.4) at a flow rate of 1 μL/min. A 30 min sampling regime is used throughout the microdialysis procedure. Following a 2 h equilibration period, 3 microdialysis samples are collected to establish basal extracellular levels of 5-HT. Guinea pigs are then dosed with vehicle (1% methyl cellulose, 1 mg/kg p.o.), paroxetine (3 mg/kg p.o.) or SB-616234-A (3, 10 or 30 mg/kg p.o.). Microdialysis samples are collected for a further 5 h following drug administration. 5-HT content of microdialysate samples is measured using high performance liquid chromatography (HPLC) with electrochemical detection (ECD). At the end of the experiment probes are removed and animals return to their home cage. Animals are re-used in a randomised cross-over design with 7 days between uses and a maximum of 4 uses per subject.

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

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7418 mL	8.7091 mL	17.4183 mL	43.5457 mL
	5 mM	0.3484 mL	1.7418 mL	3.4837 mL	8.7091 mL
	10 mM	0.1742 mL	0.8709 mL	1.7418 mL	4.3546 mL
	15 mM	0.1161 mL	0.5806 mL	1.1612 mL	2.9030 mL

Help & FAQs

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:

SB-616234-A908601-49-0Inhibitorinhibitorinhibit

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