2. GPCR/G Protein Neuronal Signaling
  3. Somatostatin Receptor
  4. SSTR3 agonist-1 TFA

SSTR3 agonist-1 TFA is a potent, orally active, and selective SSTR3 agnoist (EC50 =0.14 nM). SSTR3 agonist-1 TFA binds to SSTR3 receptor to inhibit cAMP activity. SSTR3 agonist-1 TFA decreases kidney weight and kidney cystic index (KCI) in a mouse model of autosomal dominant polycystic kidney disease (ADPKD). SSTR3 agonist-1 TFA can be used for ADPKD research.

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SSTR3 agonist-1 TFA

SSTR3 agonist-1 TFA Chemical Structure

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SSTR3 agonist-1 TFA Related Antibodies

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Description

SSTR3 agonist-1 TFA is a potent, orally active, and selective SSTR3 agnoist (EC50 =0.14 nM). SSTR3 agonist-1 TFA binds to SSTR3 receptor to inhibit cAMP activity. SSTR3 agonist-1 TFA decreases kidney weight and kidney cystic index (KCI) in a mouse model of autosomal dominant polycystic kidney disease (ADPKD). SSTR3 agonist-1 TFA can be used for ADPKD research[1].

IC50 & Target[1]

SSTR3

0.14 nM (EC50)

In Vitro

SSTR3 agonist-1 (compound 38) (20 min) TFA inhibits Forskolin (HY-15371)-stimulated cAMP accumulation in CHO-K1 cells stably expressing human SSTR3, with an EC50 of 0.14 nM[1].

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

SSTR3 agonist-1 TFA Related Antibodies
In Vivo

SSTR3 agonist-1 (compound 38) (30 and 60 mg/kg, p.o., daily for 9 days from potsnatal days (PND) 12 to 20) TFA dose dependently decreases KCI and kidney size in the ADPKD mouse model[1].

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

Animal Model: Pax8 Tet-O-Cre/Pkd1 flox mice treated with Doxycycline (HY-N0565) hyclate (50 mg/kg) to induce ADPKD[1]
Dosage: 30 and 60 mg/kg
Administration: p.o., daily for 9 days from (PND) 12 to 20
Result: Decreased KCI with a 10.7% suppression compared to the vehicle at 30 mg/kg.
Decreased KCI with a 25.2% suppression compared to the vehicle at 60 mg/kg.
Dose dependently decreased the left kidney weight/body weight (LKW/BW) ratio.
Molecular Weight

733.67

Formula

C33H38F7N5O6
Appearance

Solid

Color

Yellow to brown

SMILES

O=C(C1=C(N=C2C=C(C(OC)=CC2=C1N3CC[C@H](C)NCC3)C(F)(F)F)N4CCOCC4)N[C@@H](C)C5=CC(OC)=C(F)C=C5.O=C(O)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Purity & Documentation
References
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SSTR3 agonist-1 TFA Related Classifications

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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:

SSTR3 agonist-1Somatostatin ReceptorSSTRsSSTRSSTR3ADPKDKCIcAMPInhibitorinhibitorinhibit

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