2. GPCR/G Protein
  3. GHSR
  4. (αR,8aS)-GSK1614343

(αR,8aS)-GSK1614343 (compound 18a, d2) is a cyclized ghrelin antagonist with an pIC50 value of 8.4. (αR,8aS)-GSK1614343 shows a competitive antagonism of hGHSR1a with a mean pKb value of 8.06.

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(αR,8aS)-GSK1614343 Chemical Structure

(αR,8aS)-GSK1614343 Chemical Structure

CAS No. : 1092476-84-0

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Based on 1 publication(s) in Google Scholar

Other Forms of (αR,8aS)-GSK1614343:

(αR,8aS)-GSK1614343 Related Antibodies

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GHSR1a

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  • Customer Review

Description

(αR,8aS)-GSK1614343 (compound 18a, d2) is a cyclized ghrelin antagonist with an pIC50 value of 8.4. (αR,8aS)-GSK1614343 shows a competitive antagonism of hGHSR1a with a mean pKb value of 8.06[1].

In Vitro

(αR,8aS)-GSK1614343 (0.1-1μM) demonstrats a surmountable and competitive antagonism of hGHSR1a with a mean p KB value of 8.06[1].

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

(αR,8aS)-GSK1614343 Related Antibodies
In Vivo

(αR,8aS)-GSK1614343 (10 mg/kg; i.v. once) inhibits GH release induced by exogenous ghrelin administration[1].
(αR,8aS)-GSK1614343 (i.v. and p.o.) exhibits good oral bioavailability (F=46%), a limited clearance in blood (Clb=28 mL/min/kg) and a suitable half-life (5.0 h). In terms of rat brain penetration, a brain to blood AUC ratio of 2.2 is observed after p.o. administration of the compound at a dose of 3 mg/kg[1].
(αR,8aS)-GSK1614343 exhibits a clean profile in terms of inhibition potential for the major human CYP450 isoforms with IC50 value of ≥10 μM[1].

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

487.44

Formula

C22H23F6N5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)C1=CC(C(F)(F)F)=CC(NNC([C@@H](C2=CN=CC=C2)N3C[C@@]4([H])N(CCC4)CC3)=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (205.15 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 2.0515 mL 10.2577 mL 20.5153 mL
5 mM 0.4103 mL 2.0515 mL 4.1031 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. 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0515 mL 10.2577 mL 20.5153 mL 51.2884 mL
5 mM 0.4103 mL 2.0515 mL 4.1031 mL 10.2577 mL
10 mM 0.2052 mL 1.0258 mL 2.0515 mL 5.1288 mL
15 mM 0.1368 mL 0.6838 mL 1.3677 mL 3.4192 mL
20 mM 0.1026 mL 0.5129 mL 1.0258 mL 2.5644 mL
25 mM 0.0821 mL 0.4103 mL 0.8206 mL 2.0515 mL
30 mM 0.0684 mL 0.3419 mL 0.6838 mL 1.7096 mL
40 mM 0.0513 mL 0.2564 mL 0.5129 mL 1.2822 mL
50 mM 0.0410 mL 0.2052 mL 0.4103 mL 1.0258 mL
60 mM 0.0342 mL 0.1710 mL 0.3419 mL 0.8548 mL
80 mM 0.0256 mL 0.1282 mL 0.2564 mL 0.6411 mL
100 mM 0.0205 mL 0.1026 mL 0.2052 mL 0.5129 mL
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(αR,8aS)-GSK1614343 Related Classifications

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:

(αR,8aS)-GSK16143431092476-84-0GHSRGrowth hormone secretagogue receptorGhrelin receptorcompetitive antagonismGH releaseoral bioavailabilityCYP450Inhibitorinhibitorinhibit

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