2. Metabolic Enzyme/Protease Anti-infection
  3. Cytochrome P450 Parasite
  4. SCYX-6759

SCYX-6759 是一种口服活性的、可透过血脑屏障的抗 T. brucei 剂。SCYX-6759 可抑制 cytochrome P450 (对 2D6、2C9 和 2C19 的 IC50 值分别为 30.3、30.6 和 47.4 μM)。SCYX-6759 对 T. b. brucei427、T. b. rhodesiense STIB900 和 T. b. gambiense STIB930 均表现出强效活性，IC50 值分别为 0.07、0.038 和 0.030 μg/mL。

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SCYX-6759

SCYX-6759 Chemical Structure

CAS No. : 1222509-12-7

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SCYX-6759 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

查看 Parasite 亚型特异性产品:

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SCYX-6759 is an orally active, blood-brain barrier permeable anti-T. brucei agent. SCYX-6759 inhibits cytochrome P450 (IC50s: 30.3, 30.6, 47.4 μM for 2D6, 2C9, 2C19, respectively.) SCYX-6759 exhibits potent activity against T. b. brucei 427, T. b. rhodesiense STIB900, and T. b. gambiense STIB930, with IC50s of 0.07, 0.038 and 0.030 μg/mL, respectively[1].

IC50 & Target[1]

CYP2D6

30.3 μM (IC50)

CYP2C9

30.6 μM (IC50)

CYP2C19

47.4 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MRC5 CC50
> 64 μM
Compound: 3; SCYX-6759
Cytotoxicity against human MRC5 cells measured after 3 days by resazurin staining based fluorometric analysis
Cytotoxicity against human MRC5 cells measured after 3 days by resazurin staining based fluorometric analysis
[PMID: 34711050]
PBMC IC50
13 μM
Compound: 1L
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release incubated for 15 mins prior to LPS-challenge measured after 24 hrs by HTRF assay
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release incubated for 15 mins prior to LPS-challenge measured after 24 hrs by HTRF assay
[PMID: 24075731]
PBMC IC50
3.2 μM
Compound: 1L
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-1beta release incubated for 15 mins prior to LPS-challenge measured after 24 hrs by HTRF assay
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-1beta release incubated for 15 mins prior to LPS-challenge measured after 24 hrs by HTRF assay
[PMID: 24075731]
PBMC IC50
5.6 μM
Compound: 1L
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-6 release incubated for 15 mins prior to LPS-challenge measured after 24 hrs by HTRF assay
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-6 release incubated for 15 mins prior to LPS-challenge measured after 24 hrs by HTRF assay
[PMID: 24075731]
Peritoneal macrophage CC50
> 64 μM
Compound: 3; SCYX-6759
Cytotoxicity against mouse primary peritoneal macrophages measured after 3 days by resazurin staining based fluorometric analysis
Cytotoxicity against mouse primary peritoneal macrophages measured after 3 days by resazurin staining based fluorometric analysis
[PMID: 34711050]
分子量

339.05

Formula

C15H10BF4NO3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SCYX-6759 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

SCYX-67591222509-12-7SCYX6759SCYX 6759Cytochrome P450ParasiteCYPsT. b. bruceiT. b. rhodesienseT. b. gambienseanti-T. bruceimiceInhibitorinhibitorinhibit

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