GlpBio

YC-001

目录号: GC64384纯度: >99.00%
YC-001 是一种非视黄醛化合物，经证实对视杆细胞视蛋白 具有反向激动剂和拮抗剂活性。
YC-001
Cas No.: 748778-73-6
规格价格库存数量操作
5mg¥630.00现货
1
10mg¥1,050.00现货
1
25mg¥2,100.00现货
1
50mg¥3,360.00现货
1
10mM (in 1mL DMSO)¥693.00现货
1
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产品描述 Description

YC-001 is a non-retinal compound that has been revealed to have both inverse agonist and antagonist activity toward rod opsin [1]. Cell-based β-Gal fragment complementation activity of YC-001 (EC50: 8.7μM) showed a potency of 7.8 μM and an efficacy at 150-310% of the control activity score [1].

YC-001 (0.5, 1, 5, 10, 20, 40 μM) improves the glycosylation profile of P23H opsin mutant [1]. YC-001 (0,-1.5 μM) reversibly binds rod opsin with EC50 of 0.98 μM [1]. YC-001 (0.313, 0.625, 1.25, 2.5, 5, 10, 20, 80 μM) increases in cAMP level in a dose-dependent manner in NIH3T3 cells [1]. YC-001 rescued multiple of 27 adRP-causing RHO mutants to NIH3T3 cells. 9-cis-retinal, F5257-0462, and YC-001 rescued cell surface transport of 16, 11, and 7 mutants, respectively [2].

YC-001(40 μM, 48 h) increases the percentage of ciliary targeted RHOP23H primarily by decreasing the level of misfolded RhoP23H mutant in the ONL, which is contributed by reduced total RHOP23H protein load [2]. YC-001 improves RHO protein quality and proteostasis of the RhoP23H/+ retinae [2].YC-001 showed a TC50 (the toxic concentration of a chemical that causes the cells growing 50% as well as control) at 202 μM in RhoP23H/+ retinal explants and 64 μM in WT retinae [2].

YC-001(50 or 200 mg kg-1, i.p. )protects Abca4-/-Rdh8-/- mice from bright light-induced retinal degeneration [1].About 70 pmol per eye of YC-001 was detected at 0.5 h after i.p. injection at 200 mg kg-1 bw, increasing to 280 pmol per eye at 3 h, and then diminishing to an undetectable level by 24 h [1].YC-001 showed fast ocular clearance with a t1/2 at 0.68 hours [2].

References:
[1]:Chen Y, Chen Y, Jastrzebska B, et al. A novel small molecule chaperone of rod opsin and its potential therapy for retinal degeneration[J]. Nature communications, 2018, 9(1): 1-18.
[2]:Vats A, Xi Y, Feng B, et al. Nonretinoid chaperones improve rhodopsin homeostasis in a mouse model of retinitis pigmentosa[J]. JCI insight, 2022, 7(10).

YC-001 是一种非视黄醛化合物，经证实对视杆细胞视蛋白 [1] 具有反向激动剂和拮抗剂活性。 YC-001 的基于细胞的 β-Gal 片段互补活性（EC50:8.7μM）显示出 7.8 μM 的效力和对照活性评分的 150-310% 的功效[1]。< /p>\n

YC-001（0.5、1、5、10、20、40 μM）改善 P23H 视蛋白突变体 [1] 的糖基化特征。 YC-001 (0,-1.5 μM) 可逆地结合杆状视蛋白，EC50 为 0.98 μM [1]。 YC-001（0.313、0.625、1.25、2.5、5、10、20、80 μM）在 NIH3T3 细胞中以剂量依赖性方式增加 cAMP 水平 [1]。 YC-001 将 27 种引起 adRP 的 RHO 突变体中的多种拯救到 NIH3T3 细胞。 9-cis-retinal、F5257-0462 和 YC-001 分别挽救了 16、11 和 7 个突变体的细胞表面转运[2]。

YC-001（40 μM，48 小时）主要通过降低 ONL 中错误折叠的 RhoP23H 突变体的水平来增加纤毛靶向 RHOP23H 的百分比，这是由 RHOP23H 总蛋白负荷降低引起的[2]。 YC-001 提高 RHO 蛋白质量和 RhoP23H/+ 视网膜的蛋白质稳态 [2]。YC-001 显示 TC50（导致细胞生长 50% 的化学物质的毒性浓度，以及对照) 在 RhoP23H/+ 视网膜外植体中为 202 μM，在 WT 视网膜中为 64 μM [2]。

YC-001（50 或 200 mg kg-1，i.p.）保护 Abca4-/-Rdh8-/- 小鼠免受强光诱导的视网膜变性[1]。每只眼睛约 70 pmol在 i.p. 后 0.5 小时检测到 YC-001。以 200 mg kg-1 bw 的剂量注射，在 3 小时时每只眼睛增加到 280 pmol，然后在 24 小时内减少到检测不到的水平[1]。YC-001 显示出快速的眼部清除率，t1 /2 在 0.68 小时 [2]。

YC-001（0.5、1、5、10、20、40 μM）改善 P23H 视蛋白突变体 [1] 的糖基化特征。 YC-001 (0,-1.5 μM) 可逆地结合杆状视蛋白，EC50 为 0.98 μM [1]。 YC-001（0.313、0.625、1.25、2.5、5、10、20、80 μM）在 NIH3T3 细胞中以剂量依赖性方式增加 cAMP 水平 [1]。 YC-001 将 27 种引起 adRP 的 RHO 突变体中的多种拯救到 NIH3T3 细胞。 9-cis-retinal、F5257-0462 和 YC-001 分别挽救了 16、11 和 7 个突变体的细胞表面转运[2]。

YC-001（40 μM，48 小时）主要通过降低 ONL 中错误折叠的 RhoP23H 突变体的水平来增加纤毛靶向 RHOP23H 的百分比，这是由 RHOP23H 总蛋白负荷降低引起的[2]。 YC-001 提高 RHO 蛋白质量和 RhoP23H/+ 视网膜的蛋白质稳态 [2]。YC-001 显示 TC50（导致细胞生长 50% 的化学物质的毒性浓度，以及对照) 在 RhoP23H/+ 视网膜外植体中为 202 μM，在 WT 视网膜中为 64 μM [2]。

YC-001（50 或 200 mg kg-1，i.p.）保护 Abca4-/-Rdh8-/- 小鼠免受强光诱导的视网膜变性[1]。每只眼睛约 70 pmol在 i.p. 后 0.5 小时检测到 YC-001。以 200 mg kg-1 bw 的剂量注射，在 3 小时时每只眼睛增加到 280 pmol，然后在 24 小时内减少到检测不到的水平[1]。YC-001 显示出快速的眼部清除率，t1 /2 在 0.68 小时 [2]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Transfected 27 adRP-causing hRHO mutants to NIH3T3 cells

Preparation Method

NIH3T3 cells were seeded at 5000 cells/well and cultured in a blackwall, clear bottom, and poly-L-lysine-treated 384-well plate at 37 °C with 5% CO2 on day 1, and then transfected with the plasmids containing hRHO cDNA mutants on day 2. On day 3, cells were treated with 0.1% DMSO, 5 µM 9-cis-retinal (under dim red light), 40 µM YC-001, or 20 µM F5257-0462 in DMEM with 10% FBS for 24 h. On day 4, treated cells were fixed with 4% paraformaldehyde (PFA) in the dark for 20 min and immunostained with 15µL/well of 20 µg/mL Alexa488-conjugated B6-30 anti-RHO antibody and Hoechst 33342 (1:10,000 dilution).

Reaction Conditions

40 µM for 24 h

Applications

YC-001 rescued multiple of 27 adRP-causing RHO mutants to NIH3T3 cells. 9-cis-retinal, F5257-0462, and YC-001 rescued cell surface transport of 16, 11, and 7 mutants, respectively.
Cell experiment [1]:

Explant

Retinal explants

Preparation Method

Mice were euthanized at P15, and eyes were enucleated and incubated in Ames’ solution containing L-cysteine (0.22 mM) and papain (20 U/mL) at 37°C for 30 minutes, followed by incubation in DMEM with 10% FBS at 4°C for 5 minutes. Each eye cup was made and flattened by 4 cuts, and sclera was removed leaving only RPE attached to retina. Each retinal explant (RPE layer facing down) was cultured in a transwell in a 6-well plate with neurobasal plus medium containing 2% B27 supplement and 5 μg/mL of plasmocin at 37°C with 5% CO2 for 24 hours. The retinal explants were then treated with the same medium containing 40 μM YC-001 or DMSO. Fresh medium with the compound was changed daily.

Reaction Conditions

40 μM YC-001 for 48 h

Applications

YC-001 increases the percentage of ciliary targeted RHOP23H primarily by decreasing the level of misfolded RhoP23H mutant in the the outer nuclear layer, which is contributed by reduced total RHOP23H protein load.
Animal experiment [2]:

Animal models

Abca4−/−Rdh8−/− mice with a 129 Sv/Ev or C57BL/6 mixed background

Preparation Method

Retinal degeneration was initiated by exposing Abca4−/−Rdh8−/− mice for 30 min to white light with an intensity of 10,000 lux. Pupils of mice were dilated with 1% tropicamide 3 min before bright light exposure. YC-001 or DMSO were administered i.p. 30 min before such exposure. The effects of YC-001 were tested at two dosages: 50 and 200 mg kg−1 bw. The volume of each injection was less than 50 µL.

Dosage form

4 μg/μl, 2 μl, lateral cerebral ventricle injection

Applications

DMSO-treated mouse retinas featured significantly diminished outer nuclear layers (ONLs), indicating the loss of photoreceptor cells, YC-001-treated mice evidenced a dose-dependent protection of the ONL from light-induced damage.

References:

[1]. Vats A, Xi Y, Feng B, et al. Nonretinoid chaperones improve rhodopsin homeostasis in a mouse model of retinitis pigmentosa[J]. JCI insight, 2022, 7(10).

[2]. Chen Y, Chen Y, Jastrzebska B, et al. A novel small molecule chaperone of rod opsin and its potential therapy for retinal degeneration[J]. Nature communications, 2018, 9(1): 1-18.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
748778-73-6
分子式
C12H7ClO2S2
分子量
282.77 g/mol
溶解性
DMSO : 100 mg/mL (353.64 mM; Need ultrasonic)
保存条件
Store at -20&#176;C
General tips
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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol