WL47 TFA, a high-affinity cavolin-1 (CAV1) ligand (K_d=23 nM), is a potent disrupter of CAV1 oligomers. WL47 TFA shows selectivity for CAV1 over BSA, casein and HEWL. WL47 TFA is 80% smaller in length than the original T20 (HY-P0052) parent sequence and can be used for the study of caveolin-1 function^[1].

Kd: 23 nM (cavolin-1)^[1]

Caveolin-1 (CAV) is a monotonic membrane protein, 22 kDa, it penetrates only one leaflet of the lipid bilayer, and both the N- and C-termini remain on the cytoplasmic side. Multiple copies of CAV oligomerize can form high molecular weight complexes that bend the membrane inward to form invaginations, termed “caveolae,” of 50-100 nm in diameter.
T20 is a 36 amino acid peptide derived from gp41 and blocks HIV viral fusion with CD4⁺ T-cells. WL47 is 80% smaller in length and has 7500-fold greater affinity than the original T20 parent sequence.
In vitro, Demonstrating WL47 activity with CAV oligomers and a method for measuring the degree of oligomerization. A variant of CAV (CAV(FLV)) that spontaneously oligomerizes to form CAV nanoparticles with diameters is used to examine deoligomerization by WL47. WL47 effectively disrupts these nanoparticles, but it does not disrupt oligomerization in the presence of a reducing agent, this demonstating that WL47 function requires dimerization by disulfide bond

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

1958.32

C₈₂H₁₃₁N₂₄F₃O₂₀S₄

Lys-Leu-Arg-Met-Trp-Ser-Cys-Cys-Ser-Trp-Met-Arg-Leu-Lys

KLRMWSCCSWMRLK

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)

DMSO : 50 mg/mL (25.53 mM; Need ultrasonic)

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 (sealed storage, away from moisture and light)。-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。

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

• 1.

  请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

  Solubility: ≥ 2.5 mg/mL (1.28 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (1.28 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

  Solubility: 2.5 mg/mL (1.28 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (1.28 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

  Solubility: ≥ 2.5 mg/mL (1.28 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (1.28 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Amanda J H Gilliam,et al. Affinity-Guided Design of Caveolin-1 Ligands for Deoligomerization. J Med Chem. 2016 Apr 28;59(8):4019-25.