1. GPCR/G Protein
  2. Motilin Receptor

GSK962040 (Synonyms: Camicinal)

Cat. No.: HY-10922 Purity: 97.08%
Data Sheet SDS Handling Instructions

GSK962040(Camicinal) is a small molecule, selective motilin receptor agonist with pEC50 of 7.9.

For research use only. We do not sell to patients.
GSK962040 Chemical Structure

GSK962040 Chemical Structure

CAS No. : 923565-21-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO $385 In-stock
5 mg $350 In-stock
10 mg $500 In-stock
50 mg $1500 In-stock
100 mg $2100 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of GSK962040:

Featured Recommendations

Related Small Molecules:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK962040(Camicinal) is a small molecule, selective motilin receptor agonist with pEC50 of 7.9. IC50 Value: 7.9 (pEC50) [1] Target: Motilin Receptor in vitro: GSK962040 had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes. In rabbit gastric antrum, GSK962040 300 nmol L 1-10 μmol L 1 caused a prolonged facilitation of the amplitude of cholinergically mediated contractions, to a maximum of 248 ± 47% at 3 μmol L 1. The pEC50 values for motilin, erythromycin and GSK962040 were, respectively, 10.4 ± 0.01 (n = 770), 7.3 ± 0.29 (n = 4) and 7.9 ± 0.09 (n = 17) [1]. GSK962040 activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72, compared with [Nle13]-motilin) [2]. GSK962040 was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM [3]. in vivo: GSK962040 (5 mg free base kg 1) also produced an increase in total faecal weight over the 2-h postdose period (21.2 ± 4.5 g; P < 0.05) [1]. GSK962040 induced phasic contractions, the duration of which was dose-related (48 and 173 min for 3 and 6 mg kg 1), driven by mean plasma concentrations >1.14 μmol L 1. After the effects of GSK962040 faded, migrating motor complex (MMC) activity returned. Migrating motor complex restoration was unaffected by 3 mg kg 1 GSK962040 but at 6 mg kg 1, MMCs returned 253 min after dosing, compared with 101 min after saline (n = 5 each) [2]. he oral bioavailability (Fpo) of GSK962040 was found to be 48 ( 13%. GSK962040 shows a long lasting effect (T1/2 ) 46.9 ( 5.0 min at 3 μM) when compared with the short-lived effect of [Nle13]motilin (T1/2 ) 11.4 ( 1.5 min at 0.3 μM) [3]. GSK962040 strongly facilitated cholinergic activity in the antrum, with lower activity in fundus and small intestine only [4].

Clinical Trial
View MoreCollapse
References
Molecular Weight

424.55

Formula

C₂₅H₃₃FN₄O

CAS No.

923565-21-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 12.73 mg/mL (Need ultrasonic)

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GSK962040
Cat. No.:
HY-10922
Quantity: