SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor ofhumancathepsin Lwith anIC₅₀of 56 nM. SID 26681509 quarterhydrate inhibits in vitro propagation of malariaparasitePlasmodiumfalciparumand inhibitsLeishmaniamajorwithIC₅₀s of 15.4 μM and 12.5 μM, respectively. SID 26681509 quarterhydrate shows no inhibitory activity againstcathepsinG^[1].

After a 4 hr preincubation with cathepsin L, SID 26681509 becomes more potent, demonstrating anIC₅₀of 1.0 nM. SID 26681509 is determined to be a slow-binding and slowly reversible competitive inhibitor. Through a transient kinetic analysis for single-step reversibility, inhibition rate constants are kon = 24,000 M^-1s^-1and koff = 2.2 × 10^-5s^-1(K_i= 0.89 nM). Molecular docking studies are undertaken using the experimentally-derived X-ray crystal structure of papain/CLIK-148^[1].
SID 26681509 inhibits papain and cathepsins B, K, S, and V withIC₅₀values determined after one hour ranging from 618 nM to 8.442 μM. SID 26681509 shows no inhibitory activity against the serine protease cathepsin G^[1].
SID 26681509 inhibits cathepsin V activity with an IC₅₀value of 0.5 μM. SID 26681509 (1-30 μM) blocks high-mobility group box 1 (HMGB1)-induced TNF-α production dose dependently without altering cell viability^[2].

SID 26681509 treatment significantly improves survival in murine models of sepsis and reduces liver damage following warm liver ischemia/reperfusion (I/R) models^[2].

544.16

Solid

C₂₇H₃₃N₅O₅S.1/4H₂O

Room temperature in continental US; may vary elsewhere.

DMSO : 50 mg/mL(91.88 mM;Need ultrasonic)

Ethanol : 5 mg/mL(9.19 mM;Need ultrasonic and warming)

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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: ≥ 1.67 mg/mL (3.07 mM); Clear solution

  此方案可获得 ≥ 1.67 mg/mL (3.07 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 16.7 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