ChemicalBook > CAS DataBase List > TG6-10-1

TG6-10-1

Product Name
TG6-10-1
CAS No.
1415716-58-3
Chemical Name
TG6-10-1
Synonyms
CS-2074;TG6-10-1;TG6-10-1, >98%;TG6-10-1, 10 mM in DMSO;Prostaglandin EP2 Receptor Antagonist, TG6-10-1;(E)-N-(2-(2-(trifluoromethyl)-1H-indol-3-yl)ethyl) -3-(3,4,5-trimethoxyphenyl)acrylamide;2-Propenamide, N-[2-[2-(trifluoromethyl)-1H-indol-1-yl]ethyl]-3-(3,4,5-trimethoxyphenyl)-, (2E)-
CBNumber
CB33041469
Molecular Formula
C23H23F3N2O4
Formula Weight
448.43
MOL File
1415716-58-3.mol
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TG6-10-1 Property

Boiling point:
631.8±55.0 °C(Predicted)
Density 
1.24±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMF: 50 mg/ml; DMSO: 30 mg/ml; Ethanol: 5 mg/ml
form 
A crystalline solid
pka
13.84±0.46(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H317May cause an allergic skin reaction

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
5.05765
Product name
Prostaglandin EP2 Receptor Antagonist, TG6-10-1
Packaging
10 mg
Price
$259
Updated
2025/07/31
Cayman Chemical
Product number
23444
Product name
TG6-10-1
Purity
≥98%
Packaging
1mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
23444
Product name
TG6-10-1
Purity
≥98%
Packaging
5mg
Price
$151
Updated
2024/03/01
Cayman Chemical
Product number
23444
Product name
TG6-10-1
Purity
≥98%
Packaging
10mg
Price
$231
Updated
2024/03/01
Cayman Chemical
Product number
23444
Product name
TG6-10-1
Purity
≥98%
Packaging
25mg
Price
$530
Updated
2024/03/01
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TG6-10-1 Chemical Properties,Usage,Production

Uses

TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors[1].

Biological Activity

Primary Target
EP2', 'Reversible: yes

Synthesis

20329-98-0

1415601-84-1

1415716-58-3

General procedure for the synthesis of (E)-N-(2-(2-(2-(trifluoromethyl)-1H-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide (15d): Compound 13b (480 mg, 2.1 mmol) was dissolved in dichloromethane (10 mL) at room temperature, and sequentially added (E)-3-(3,4,5-trimethoxyphenyl ) acrylic acid (14a) (504 mg, 2.1 mmol), 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDCI) (523 mg, 2.73 mmol) and N,N-dimethylaminopyridine (DMAP) (10 mg). The reaction mixture was stirred at room temperature for 8 hours. Upon completion of the reaction, the reaction was quenched with water (10 mL) and the product was extracted with ethyl acetate (20 mL × 3). The organic phases were combined and washed sequentially with 1% HCl (10 mL), saturated NaHCO3 solution (10 mL), water (20 mL), and brine (20 mL), then dried with anhydrous Na2SO4. After concentration under reduced pressure, the crude product was purified by silica gel column chromatography with the eluent being a hexane solution of 0-35% ethyl acetate to give the target product 15d (700 mg, 74% yield). The 1H NMR (CDCl3) data of product 15d: δ 7.59 (d, J = 8 Hz, 1H), 7.54 (d, J = 8.4 Hz, 1H), 7.50 (d, J = 15.2 Hz, 1H), 7.27 (q, J = 7.2 Hz, 1H), 7.1 (t, J = 7.2 Hz, 1H), 6.89 (s, 1H), 6.63 (s, 2H), 6.4 (t, J = 6 Hz, 1H), 6.25 (d, J = 15.2 Hz, 1H), 4.4 (t, J = 6.4 Hz, 1H), 3.8 (s, 3H), 3.76 (s, 6H), 3.69 (q, J = 6.4 Hz, 2H). lCMS (ESI) analysis: λ254 nm, MS purity > 95%; m /z 449 [M + H]+. Calculated elemental analysis (C23H23F3N2O4): C, 61.60; H, 5.17; N, 6.25; measured values: C, 61.34; H, 5.10; N, 6.16.

in vivo

TG6-10-1 (5 mg/kg; i.p.; 4-30 hours) improves survival, accelerates recovery of lost weight, and improves functional recovery following status epilepticus (SE) [1].

Animal Model:C57BL/6 mice (pilocarpine-induced SE)[1]
Dosage:5 mg/kg
Administration:Intraperitoneal injection; 4, 21, 30 hours
Result:A significant increase in survival and accelerating the recovery of lost weight in post-SE mice.

References

[1] Jiang J, et al. Inhibition of the prostaglandin receptor EP2 following status epilepticus reduces delayed mortality and brain inflammation. Proc Natl Acad Sci U S A. 2013 Feb 26;110(9):3591-3596. DOI:10.1073/pnas.1218498110
[2] Kang X, et al. Cyclooxygenase-2 contributes to oxidopamine-mediated neuronal inflammation and injury via the prostaglandin E2 receptor EP2 subtype. Sci Rep. 2017 Aug 25;7(1):9459. DOI:10.1038/s41598-017-09528-z

TG6-10-1 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from TG6-10-1 manufacturers

Career Henan Chemical Co
Product
TG6-10-1 1415716-58-3
Price
US $1.00/ASSAYS
Min. Order
1ASSAYS
Purity
95%~99%
Supply Ability
per week:100kg
Release date
2019-09-05

1415716-58-3, TG6-10-1Related Search:


  • TG6-10-1
  • (E)-N-(2-(2-(trifluoromethyl)-1H-indol-3-yl)ethyl) -3-(3,4,5-trimethoxyphenyl)acrylamide
  • CS-2074
  • TG6-10-1, >98%
  • 2-Propenamide, N-[2-[2-(trifluoromethyl)-1H-indol-1-yl]ethyl]-3-(3,4,5-trimethoxyphenyl)-, (2E)-
  • TG6-10-1, 10 mM in DMSO
  • Prostaglandin EP2 Receptor Antagonist, TG6-10-1
  • 1415716-58-3
  • api
  • Inhibitors