1. GPCR/G Protein
  2. GPR40
  3. GW-1100

GW-1100 

Cat. No.: HY-50691 Purity: ≥97.0%
Handling Instructions

GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9.

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

GW-1100 Chemical Structure

GW-1100 Chemical Structure

CAS No. : 306974-70-9

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 81 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 81 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 71 In-stock
Estimated Time of Arrival: December 31
10 mg USD 134 In-stock
Estimated Time of Arrival: December 31
50 mg USD 562 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 14 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GW-1100 purchased from MCE. Usage Cited in: J Endocrinol. 2019 Feb 1;240(2):195-214.

    Western analysis of p-Akt, t-Akt and IRS2 in the treatment of STZ, GW1100 or Vin.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9.

    IC50 & Target

    pIC50: 6.9 (GPR40)[1]

    In Vitro

    GW-1100 (GW1100) dose dependently inhibits GPR40-mediated Ca2+ elevations stimulated by GW9508 and linoleic acid (pIC50 values of 5.99±0.03 and 5.99±0.06, respectively). GW-1100 at a concentration of 1 μM produces a significant rightward shift in the concentration-response curve to GW9508 (pEC50=7.17±0.08 in the absence and pEC50=6.79±0.09 in the presence of 1 μM GW-1100; P<0.05; n=3). At concentrations of GW-1100 of 3 μM and higher a significant decrease in the maximal response is observed with a continuing rightward shift in the pEC50 response[2]. GW-1100 (GW1100) reduces FFAR1 ligand-induced intracellular calcium in CHO-K1/bFFAR1 cells and neutrophils. CHO-K1/bFFAR1 cells are incubated for 15 min with 10 μM GW1100 or vehicle (0.1% DMSO) and then stimulated with vehicle, oleic acid, linoleic acid or GW9508. GW-1100 significantly reduces the increase in intracellular calcium induced by 300 μM oleic acid (AUC(60-150 s), p<0.05), 100 μM linoleic acid (AUC(60-150 s), p<0.05) and 10 μM GW9508 (AUC(60-150 s), p<0.05)[3].

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

    In Vivo

    The intracerebroventricular injection of DHA (50 µg) and GW9508 (1.0 µg), a GPR40-selective agonist, significantly reduces mechanical allodynia and thermal hyperalgesia at day 7, but not at day 1, after CFA injection. These effects are inhibited by intracerebroventricular pretreatment with GW-1100 (10 µg), a GPR40 antagonist[4].

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

    Molecular Weight

    520.58

    Formula

    C₂₇H₂₅FN₄O₄S

    CAS No.
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (96.05 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9209 mL 9.6047 mL 19.2093 mL
    5 mM 0.3842 mL 1.9209 mL 3.8419 mL
    10 mM 0.1921 mL 0.9605 mL 1.9209 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    50% PBS

      Solubility: 5 mg/mL (9.60 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    • 3.

      Add each solvent one by one:  1% DMSO    99% saline

      Solubility: 0.06 mg/mL (0.12 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [3]

    CHO-K1/bFFAR1 or CHO-K1/pcDNA3.1 cells (2×106 cells/2 mL) are loaded with 2.5 μM Fura-2AM fluorescent indicator dye in recording buffer (10 mM HEPES, 140 mM NaCl, 2 mM CaCl2, 21 mM MgCl2, 25 mM KCl, 10 mM glucose, pH 7.4) for 30 min, washed three times with recording buffer, and returned to the incubator for 10 min. Cells are incubated with different concentrations of propionic acid (1, 10 and 30 mM), oleic acid (0-500 μM), linoleic acid (0-200 μM), GW9508 (0-100 μM), ionomycin (2 μM), thapsigargin (2 μM) or vehicle (0.1% DMSO). The fatty acid concentrations used in all experiments are in the range of concentrations of healthy and peripartum cows. In another set of experiments, cells are incubated with either 10 μM GW-1100 for 15 min, 2 μM U73122 for 3 min or vehicle (0.1% DMSO) for 15 min and then stimulated with either 300 μM oleic acid, 100 μM linoleic acid or 10 μM GW9508. Cellular fluorescence (Ca2+) is measured at 509 nm emission with 340/380 nm dual wavelength excitation using a LS55 spectrofluorimeter. Cuvette temperatures are maintained at 37°C with constant stirring[3].

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

    Animal Administration
    [4]

    Mice[4]
    Male ddY mice (age, 4 weeks) are housed in cages at 23-24°C with a 12-h light-dark cycle (lights from 8 am to 8 pm) and food and waterad libitum. DHA (50 µg/mouse), the selective GPR40-agonist GW9508 (1.0-25 µg/mouse) and the GPR40 antagonist GW1100 (1-10 µg/mouse) are dissolved in 1% DMSO and the solution is diluted with saline before von Frey testing (1% DMSO final concentration). The doses of GW9508 are chosen based upon our previous publication, whereas GW-1100 is selected on the basis of previous reports and our preliminary experiments. Under a non-anesthetized state, DHA and GW9508 are administered via the intracerebroventricular (i.c.v.) route 10 min before CFA injection, and GW1100 is administered via the i.c.v. route 10 min before GW9508 injection. Flavopiridol (5 and 15 nmol/mouse), a cyclin-dependent kinase inhibitor, is administered by i.c.v. injection into the left lateral ventricle of the mice twice a day (at 9:00 and 19:00) after CFA treatment.

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

    References
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    Product Name:
    GW-1100
    Cat. No.:
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