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重組肝臟酵素 Gentest® Supersomes®
Gentest® Supersomes® 是世界公認的 重組細胞色素 P450(CYP)與其他代謝酵素 產品,專為體外代謝研究(ADME)設計。這些酵素由杆狀病毒轉染昆蟲細胞製備,提供比典型人肝微粒體更高的催化活性,是藥物代謝機制與藥物交互作用評估的重要工具。
Gentest® Supersomes®
  • Gentest® Supersomes®
  • 產品細節 Ⅰ
  • 產品細節 ⅠⅠ

★ 高催化活性Supersomes® 的酵素活性通常比人類肝微粒體高出約 6 倍,有助於提高反應線性階段時間與產物生成效率,適合慢代謝化合物的深入研究。

★ 全面酵素組合提供最完整的一組 CYP 酵素,可覆蓋主要 Phase I 代謝途徑,並可延伸至 Phase II 路徑。

★ 模擬天然酵素動力學與人肝與其他器官天然酵素相比,Supersomes® 的酵素動力學表現一致,因此更接近 in vivo 代謝情況。

 

優質重組 CYP 酵素

CYP 代謝酵素

Supersomes® 含最完整的 CYP450 系列,可搭配 NADPH 還原酶,提供強大催化能力。

 

請詳見《產品細節》

除了 CYP,也提供以下重組酵素:

  • UGTUDP-glucuronosyl transferases
  • FMOFlavin-containing monooxygenases
  • MAOMonoamine oxidases
  • AOAldehyde oxidase
  • NATSoluble N-acetyltransferases
  • CESCarboxylesterases

常見用途(Applications

 

高通量藥物交互作用篩選(High-throughput DDI screening 

慢代謝化合物代謝研究(Slow metabolizing compounds       

代謝物生成與結構鑑定(Metabolite identification

反應表型分析(Reaction phenotyping

酵素抑制與動力學分析(Enzyme inhibition & kinetics

評估前體藥物(Pro-drug)與 CYP 代謝清除通路(CYP pathways

 

All suitable for regulatory ADME studies and reaction phenotyping.

 

Supersomes® enable efficient metabolite formation with a long linear time course and high catalytic activity, making them ideal for screening slow-metabolizing drug compounds.

 

Human P450 Enzymes

Catalog Number

Description

P450 Content

(nmol)

Qty

(mL)

456211

Human CYP1A1 + reductase

0.5

0.5

456203

Human CYP1A2 + reductase

0.5

0.5

456220

Human CYP1B1 + reductase

0.5

0.5

456204

Human CYP2A6 + reductase

1

0.5

456254

Human CYP2A6 + reductase + b5

0.5

0.5

456210

Human CYP2B6 + reductase

0.5

0.5

456255

Human CYP2B6 + reductase + b5

0.5

0.5

456222

Human CYP2C18 + reductase

0.5

0.5

456219

Human CYP2C19 + reductase

0.5

0.5

456259

Human CYP2C19 + reductase + b5

0.5

0.5

456212

Human CYP2C8 + reductase

1

0.5

456252

Human CYP2C8 + reductase + b5

0.5

0.5

456218

Human CYP2C9*1 (Arg144) + reductase

1

0.5

456258

Human CYP2C9*1 (Arg144) + reductase + b5

0.5

0.5

456217

Human CYP2D6*1 (Val374) + reductase

0.5

0.5

456206

Human CYP2E1 + reductase + b5

1

0.5

456264

Human CYP2J2 + reductase + b5

0.5

0.5

456207

Human CYP3A4 + reductase

1

0.5

456202

Human CYP3A4 + reductase + b5

0.5

0.5

456235

Human CYP3A5 + reductase

1

0.5

456256

Human CYP3A5 + reductase + b5

0.5

0.5

456237

Human CYP3A7 + reductase + b5

0.5

0.5

456221

Human CYP4A11 + reductase

0.5

0.5

456272

Human CYP4F2 + reductase + b5

0.5

0.5

456273

Human CYP4F3A + reductase + b5

0.25

0.5

456274

Human CYP4F3B + reductase + b5

0.5

0.5

456275

Human CYP4F12 + reductase + b5

0.5

0.5

456260

Human CYP19 (aromatase) + reductase

0.5

0.5

 

 

 

 

Discovery also offers a range of non-CYP Supersomes® enzymes.

 

Human UGT Enzymes

Catalog Number

Description

Protein Content

(mg/mL)

Qty

(mL)

456400

UGT control microsomes

5

0.5

456411

Human UGT1A1

5

0.5

456413

Human UGT1A3

5

0.5

456414

Human UGT1A4

5

0.5

456416

Human UGT1A6

5

0.5

456407

Human UGT1A7

5

0.5

456418

Human UGT1A8

5

0.5

456419

Human UGT1A9

5

0.5

456410

Human UGT1A10

5

0.5

456424

Human UGT2B4

5

0.5

456427

Human UGT2B7

5

0.5

453323

Human UGT2B10

5

0.5

456435

Human UGT2B15

5

0.5

456437

Human UGT2B17

5

0.5

UGT = UDP-glucuronosyltransferase

 

 

Other Human Metabolic Enzymes

Catalog Number

Description

Protein Content

(mg/mL)

Qty

(mL)

453320 Human CES1b

5

0.5

453321 Human CES1c

5

0.5

453322 Human CES2

5

0.5

453322 Human FMO1

5

0.5

456233 Human FM03

5

0.5

456245 Human FM05

5

0.5

456280 Monoamine Oxidase (MAO) Control

5

0.5

456283 Human Monoamine Oxidase A (MAO-A)

5

0.5

456284 Human Monoamine Oxidase B (MAO-B)

5

0.5

456800 Human Control Cystosol

5

0.5

456801 Human Aldehyde Oxidase (AOX1)

5

0.5

FMO = Flavin-containing monooxygenase

Gentest® Supersomes® Controls, Cofactors, and Buffers

Analysis of Cytochrome P450, UGT, and MAO isoform-specific metabolism requires use of the appropriate control preparation in order to eliminate the possibility of metabolism by enzymes native to the cell lines.

 

Catalog Number

Supersomes®Descriptions

Protein Concentration

(mg/mL)

Qty(mL)

456200

Insect cell control for Gentest® Supersomes® enzymes baculovirus-insect cell-expressed (BTl-TN-5B1-4 cells)

5

1.5

456201

Insect cell control for Gentest® Supersomes® enzymes baculovirus-insect cell-expressed (BTl-TN-5B1-4 cells)

5

0.5

456400

Human UGT Insect Control for Gentest® UGT-expressing Supersomes®

5

0.5

456280

MAO Insect Control for Gentest® MAO-expressing Supersomes®

5

0.5

456244

Human P450 reductase and b5 control for baculovirus expressed (BTl-TN-5B1-4 cells)

5

0.5

Catalog Number

Cofactor Description

Qty(mL)

451220

NADPH Regenerating system — Solution A (NADPand GIc-6-PO4)

5

451200

NADPH Regenerating system — Solution B (G6PDH)

1

451300

UGT Reaction mix — Solution A (UDPGA)

2

451320

UGT Reaction mix — Solution B (Alamethicin)

5

Catalog Number

Buffer Description

Qty(mL)

451201

Phosphate buffer (pH 7.4)

500