1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. RAR/RXR
  3. KCL-286

KCL-286  (Synonyms: C286)

目录号: HY-111573 纯度: 98.93%
COA 产品使用指南 技术支持

KCL-286 (C286) 是一种口服有效,可以透过血脑屏障的视黄酸受体 (RAR) β2 激动剂 (EC50 = 1.9 nM)。KCL-286 靶向 RARβ2,对 RAR α (EC50 = 26 nM) 和 RAR γ (EC50 = 11 nM) 具有良好的选择性。KCL-286 可激活受损神经元中的 RARβ2。KCL-286 通过中枢神经系统的抑制性环境诱导脊髓神经和感觉神经的轴突再生,调节神经炎症和细胞外基质分子。KCL-286 可以通过神经元分泌核心蛋白聚糖来调节 CSPG 的表达,从而促进髓鞘形成并帮助轴突生长。KCL-286 可用于脊髓损伤和创伤性神经损伤等领域的研究。

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KCL-286 Chemical Structure

KCL-286 Chemical Structure

CAS No. : 1952276-71-9

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10 mg ¥3850
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Customer Review

查看 RAR/RXR 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KCL-286 (C286) is an orally active and brain-penetrant retinoic acid receptor (RAR) β2 agonist (EC50 = 1.9 nM). KCL-286 targets RARβ2 with good selectivity over RAR α (EC50 = 26 nM) and RAR γ (EC50 = 11 nM). KCL-286 activates RARβ2 in the injured neurons. KCL-286 induces axonal regeneration of both spinal and sensory nerves through the inhibitory environment of the CNS, modulates neuroinflammation and extracellular matrix molecules. KCL-286 can modulate the expression of CSPGs by neuronal secretion of decorin which promotes myelination and aids axonal growth. KCL-286 can be studied in research for area such as spinal cord injury and traumatic nerve injury[1][3].

IC50 & Target

RAR α (EC50 = 26 nM);RAR β (EC50 = 1.9 nM);RAR γ (EC50 = 11 nM)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
COS-7 EC50
1.9 nM
Compound: 10
Transactivation of GAL4-fused mouse RARbeta-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay
Transactivation of GAL4-fused mouse RARbeta-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay
[PMID: 30792038]
COS-7 EC50
13 nM
Compound: 10
Transactivation of GAL4-fused mouse RARgamma-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay
Transactivation of GAL4-fused mouse RARgamma-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay
[PMID: 30792038]
COS-7 EC50
26 nM
Compound: 10
Transactivation of GAL4-fused mouse RARalpha-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay
Transactivation of GAL4-fused mouse RARalpha-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay
[PMID: 30792038]
HEK293 EC50
2.05 nM
Compound: 10
Transactivation of GAL4 DBD-fused human RARbeta-LBD expressed in HEK293 cells by beta-lactamase reporter gene based assay
Transactivation of GAL4 DBD-fused human RARbeta-LBD expressed in HEK293 cells by beta-lactamase reporter gene based assay
[PMID: 30792038]
体外研究
(In Vitro)

KCL-286 (0.1 μM,72 小时) 显著增加神经突密度和突触数量,从而激活 RARβ2[2]

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

体内研究
(In Vivo)

KCL-286 (3 mg/kg,口服,每隔一天一次,持续 4 周) 可调节多种再生途径,并恢复损伤大鼠模型中的 ECM 水平和细胞粘附分子[2]
KCL-286 (3 mg/kg,口服,每隔一天一次,持续 4 周) 可改善中度胸椎 SC 挫伤大鼠模型中的后肢运动功能[2]
KCL-286 (3 mg/kg,口服,每隔一天一次,持续 4 周) 在 C5-T1 背根撕脱伤大鼠模型中,3 周后运动和感觉功能完全恢复[2]

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

Animal Model: Non-injured or avulsed male Sprague-Dawley rats[2]
Dosage: 3 mg/kg, every other days for 4 weeks
Administration: Oral gavage (p.o.)
Result: Resulted in 82 genes presenting a return to their basal level and 99 genes being strongly upregulated in injured model.
Resulted in 58 genes returning to their basal level after being significantly downregulated under injured conditions.
Significantly modified genes associated with ECM, paths within this signaling complex were both upregulated (those pertaining to the modulation of the cholinergic system, ion transport, and ion channels) or downregulated by the drug after injury.
Highly upregulated the ligand-gated ion channel.
Regulated the G-protein coupled receptor signaling cascades and G-protein coupled receptor protein pathways and chemokine signalling.
Upregulated RARβ in the cell bodies and axons of all neuron subtypes.
Animal Model: Moderate thoracic SC contusion male Sprague-Dawley rat model[2]
Dosage: 3 mg/kg, every other days for 4 weeks
Administration: Oral gavage (p.o.)
Result: Significantly reduced the tissue loss that progressively occurs at sub-acute and chronic stages following the injury.
Significantly reduced gliosis, shown by reduction in OX42 expression and neuronal loss assessed by neuronal nuclear protein (NeuN) levels.
Significantly lowered the expression of reactive astrocytes Glial fibrillary acidic protein and microglia Ionized Calcium Binding Adaptor Molecule 1.
Significantly upregulated decorin expression and lowered CSPGs in contused rats.
分子量

334.33

Formula

C19H14N2O4

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 6.25 mg/mL (18.69 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9911 mL 14.9553 mL 29.9106 mL
5 mM 0.5982 mL 2.9911 mL 5.9821 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 0.62 mg/mL (1.85 mM); 澄清溶液

    此方案可获得 ≥ 0.62 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 6.2 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9911 mL 14.9553 mL 29.9106 mL 74.7764 mL
5 mM 0.5982 mL 2.9911 mL 5.9821 mL 14.9553 mL
10 mM 0.2991 mL 1.4955 mL 2.9911 mL 7.4776 mL
15 mM 0.1994 mL 0.9970 mL 1.9940 mL 4.9851 mL
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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产品名称:
KCL-286
目录号:
HY-111573
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