2. Metabolic Enzyme/Protease
  3. Dipeptidyl Peptidase
  4. Anagliptin

Anagliptin  (Synonyms: SK-0403)

製品番号: HY-14877 純度: ≥97.0%
COA 取扱説明書

Anagliptin (SK-0403) is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively.

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Anagliptin 構造式

Anagliptin 構造式

CAS 番号 : 739366-20-2

容量 価格（税別） 在庫状況 数量
Solution
10 mM * 1 mL in DMSO USD 169 在庫あり
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 169 在庫あり
Estimated Time of Arrival: December 31
Solid
5 mg USD 154 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 264 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1045 在庫あり
Estimated Time of Arrival: December 31
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 3 publication(s) in Google Scholar

Other Forms of Anagliptin:

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製品説明

Anagliptin (SK-0403) is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively[1].

IC50 & Target

DPP-4

3.8 nM (IC50)

DPP-9

60 nM (IC50)

DPP-8

68 nM (IC50)

体外実験

Anagliptin (SK-0403) (0-100 μM; 24 h) attenuates s-DPP-4-induced smooth muscle cells proliferation[2].
Anagliptin (100 μM; 10 min) reduces TNF-α production in cultured monocytes[2].
Anagliptin (0.001-10 μM; 24 h) significantly suppresses sterol regulatory element‐binding protein activity in HepG2 cells (21% decrease)[3].

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

Cell Proliferation Assay[2]

Cell Line: Rat smooth muscle cells (SMC)
Concentration: 1, 10 and 100 μM
Incubation Time: 24 h
Result: Attenuated s-DPP-4-induced SMC proliferation in a dose-dependent manner. Inhibited LPS-induced ERK phosphorylation and markedly suppressed LPS-induced nuclear translocation of NF-κBp65.

Western Blot Analysis[2]

Cell Line: Rat smooth muscle cells (SMC)
Concentration: 100 μM
Incubation Time: 10 min
Result: Blocked the early- but not the late-phase ERK phosphorylation induced by s-DPP-4.
体内実験

Anagliptin (SK-0403) (0.3%; in diet; 16 weeks) reduces atherosclerotic lesion and does not increase the number of circulating EPCs in apoliporotein E (apoE)-deficient mice[2].
Anagliptin (0.3%; in diet; 4 weeks) exhibits a lipid‐lowering effect in a hyperlipidemic mice model[3].

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

Animal Model: Male apoliporotein E (apoE)-deficient mice[2]
Dosage: 0.3%
Administration: In diet, 16 weeks
Result: Reduced DPP-4 activity in the plasma as expected and did not affect food consumption or body weight gain. Significantly reduced total cholesterol level, especially VLDL and LDL-C without affecting triglyceride level. Also decreased the α-SMA-positive area within the individual plaque.
Animal Model: Male low‐density lipoprotein receptor‐deficient mice (B6.129S7‐Ldlrtm1Her/J)[3]
Dosage: 0.3%
Administration: In diet, 4 weeks
Result: Significantly decreased the plasma total cholesterol (14% reduction) and triglyceride levels (27% reduction). Significantly decreased low‐density lipoprotein cholesterol and very low‐density lipoprotein cholesterol. Sterol regulatory element‐binding protein‐2 messenger ribonucleic acid expression level was significantly decreased at night.
Animal Model: Male Sprague–Dawley rats and Beagle dogs[1]
Dosage: 0.2, 0.5, 1 and 10 mg/kg
Administration: Oral or intravenous administration (Pharmacokinetic Studies)
Result: Selected PK parameters of Anagliptin hydrochloride in rats and dogs[1]
Compound Species CLtot
(l/h/kg)		 Vdss
(l/h/kg)		 Cmaxc
(ng/ml)		 Tmaxc
(h)		 T1/2
(h)		 AUC
(ng/h/ml)		 BA
(%)
Anagliptin hydrochloridea Rat 2.00 (iv) 0.68 (iv) 309 (62) (po) 0.8 (2.3) (po) 1.9 (po) 1160 (po) 23 (po)
Dog 0.65 (iv) 0.83 (iv) 261 (po) 1.5 (po) 1.0 (po) 824 (po) 100 (po)

aAnagliptin hydrochloride dose in rats, 1 mg/kg, iv (n = 3); 10 mg/kg, po (n = 3). 4a dose in dogs, 0.2 mg/kg, iv (n = 3); 0.5 mg/kg, po (n = 2). cValues in parentheses were obtained at a dose of 3 mg/kg (n = 3).
臨床実験
分子量

383.45

Appearance

Solid

分子式

C19H25N7O2
CAS 番号
SMILES

O=C(C1=CN2C(N=C1)=CC(C)=N2)NCC(C)(NCC(N3[[email protected]](C#N)CCC3)=O)C
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (260.79 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6079 mL 13.0395 mL 26.0790 mL
5 mM 0.5216 mL 2.6079 mL 5.2158 mL
10 mM 0.2608 mL 1.3040 mL 2.6079 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

*All of the co-solvents are available by MCE.
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参考文献
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Keywords:

Anagliptin739366-20-2SK-0403SK0403SK 0403Dipeptidyl PeptidaseDPPatherosclerosissmooth muscle celllipid‐loweringSMCDPP-8DPP-4Inhibitorinhibitorinhibit

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