1. Membrane Transporter/Ion Channel
  2. SGLT
  3. TA-1887

TA-1887 (JNJ-39933673) is a highly potent, selective and orally active SGLT2 inhibitor (IC50: 1.4 nM) with antihyperglycemic effects. TA-1887 can be used in the research of diabetes.

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

TA-1887 Chemical Structure

TA-1887 Chemical Structure

CAS No. : 1003005-29-5

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Description

TA-1887 (JNJ-39933673) is a highly potent, selective and orally active SGLT2 inhibitor (IC50: 1.4 nM) with antihyperglycemic effects. TA-1887 can be used in the research of diabetes[1][2].

IC50 & Target[1]

SGLT2

1.4 nM (IC50)

SGLT1

230 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
CHO-K1 EC50
1.9 nM
Compound: 6
Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as reduction in [14C]-alpha-methylglucopyranoside uptake after 2 hrs by liquid scintillation counting
Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as reduction in [14C]-alpha-methylglucopyranoside uptake after 2 hrs by liquid scintillation counting
[PMID: 21090651]
In Vivo

TA-1887 (30 mg/kg, oral administration, rats) induces glucose excretion over a 24 h period of 2502 mg per 200 g body weight[1].
TA-1887 (3 mg/kg, oral administration) reduces blood glucose levels without influencing food intake in hyperglycemic high-fat diet-fed KK (HF-KK) mice[1].
TA-1887 (30 mg/kg/day, oral gavage for 2 weeks) significantly reduces GFR (glomerular filtration rate) in BSA-overloaded diabetic mice[2].
TA-1887 (0.01% w/w in chow, HF diets fed mice) antagonizes diabetic cachexia and decreases mortality in diabetic mice[3].

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

Animal Model: Sprague-Dawley rats[1]
Dosage: 30 mg/kg
Administration: Oral administration
Result: Induced extensive UGE (urinary glucose excretion) through continuous suppression of renal glucose reuptake.
Animal Model: BSA-overloaded diabetic mice[2]
Dosage: 30 mg/kg
Administration: Oral gavage for 2 weeks
Result: Suppressed the induction of TGF‐β2 level in vehicle‐treated BSA‐overloaded diabetic mice.
Suppressed COL3 gene levels.
Animal Model: Male Sprague-Dawley rats (pharmacokinetic assay)[1]
Dosage: 3 mg/kg (i.v.), 10 mg/kg (p.o.)
Administration: Oral administration (p.o.), intravenous injection (i.v.)
Result: Pharmacokinetic (PK) parameters of TA-1887.
Parameters dose (mg/kg) Cmax (ng/mL) t1/2 (h) F (%)
TA-18873 (i.v.) 3.9
TA-18873 10 (p.o.) 2723 3.9 78
Molecular Weight

427.47

Formula

C24H26FNO5

CAS No.
SMILES

FC1=C2C(N([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)C=C2CC4=CC=C(C5CC5)C=C4)=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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TA-1887 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.

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Product Name:
TA-1887
Cat. No.:
HY-12608
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