| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| ln Vitro |
G-1 is a selective GPR30 coagulant that has a high affinity and is nonsteroidal, with a Ki of 11 nM [1]. G-1 treatment (10 μM and 100 μM) for 48 and 72 hours dramatically inhibited cell proliferation (P<0.001). G-1's IC50 value at 72 hours was determined to be 20 μM. G-1 treatment of A549 cells at a dose of 20 μM resulted in a considerable increase in cells and a persistent anti-proliferative impact (P<0.001). After receiving G-1 therapy for 24 hours, cell cycle examination of H295R cells revealed that the cells were in the G2 phase of their life cycle. G-1 decreases Bcl-2 while also expressing Bax[3].
|
|---|---|
| ln Vivo |
The Basso S Scale (BMS) score of the G-1 group was substantially greater (P<0.05) than that of the other groups, according to the results obtained 14 days after the injury. This group had fewer positive cells than the other groups (P<0.05), and there was no difference when compared (P>0.05)[1]. Beginning on day 14 of therapy, the G-1 medication resulted in a statistically significant decrease in the volume of the tumor, and after three weeks of treatment, the tumor weight of transplanted tumors was significantly lower than that of animals receiving a vehicle treatment [3].
|
| References |
|
| Additional Infomation |
G-1 is an agonist.
G Protein-coupled Estrogen Receptor Agonist LNS8801 is an orally bioavailable selective agonist of the G protein-coupled estrogen receptor (G protein-coupled estrogen receptor 1; GPER; GPER1; GPR30), with potential immunomodulating and antineoplastic activities. Upon oral administration, LNS8801 targets, binds to and activates GPER. This activates GPER-mediated signaling and suppresses the expression of various tumor-associated genes, such as c-Myc and programmed cell death-ligand 1 (PD-L1). This leads to an inhibition of tumor cell proliferation. GPER activation may also induce immune memory. GPER is a membrane protein and a member of the G-protein coupled receptors (GPCRs) that are widely distributed in various tissues. GPER is a tumor suppressor in a wide range of cell cancer types. |
| Molecular Formula |
C21H18BRNO3
|
|---|---|
| Molecular Weight |
412.28
|
| Exact Mass |
411.046
|
| Elemental Analysis |
C, 61.18; H, 4.40; Br, 19.38; N, 3.40; O, 11.64
|
| CAS # |
881639-98-1
|
| PubChem CID |
5322399
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
529.6±50.0 °C at 760 mmHg
|
| Flash Point |
274.1±30.1 °C
|
| Vapour Pressure |
0.0±1.4 mmHg at 25°C
|
| Index of Refraction |
1.637
|
| LogP |
4.37
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
26
|
| Complexity |
596
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
BrC1C=C2OCOC2=CC=1[C@@H]1NC2C=CC(=CC=2[C@@H]2C=CC[C@H]12)C(=O)C
|
| InChi Key |
VHSVKVWHYFBIFJ-HKZYLEAXSA-N
|
| InChi Code |
InChI=1S/C21H18BrNO3/c1-11(24)12-5-6-18-15(7-12)13-3-2-4-14(13)21(23-18)16-8-19-20(9-17(16)22)26-10-25-19/h2-3,5-9,13-14,21,23H,4,10H2,1H3/t13-,14+,21-/m1/s1
|
| Chemical Name |
1-[(3aS,4R,9bR)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]ethanone
|
| Synonyms |
G1; G 1; G-1
|
| HS Tariff Code |
2934.99.03.00
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~121.28 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.06 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4255 mL | 12.1277 mL | 24.2554 mL | |
| 5 mM | 0.4851 mL | 2.4255 mL | 4.8511 mL | |
| 10 mM | 0.2426 mL | 1.2128 mL | 2.4255 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
