UK-370106 is a potent and highly selectiveMMP-3(IC₅₀of 23 nM) andMMP-12(IC₅₀of 42 nM) inhibitor with >1200-fold higher potency thanMMP-1,MMP-2,MMP-9, andMMP-14, and about 100-fold thanMMP-13andMMP-8. UK-370106 potently inhibits cleavage of [³H]-fibronectin byMMP-3(IC₅₀of 320 nM) and has little effect on keratinocyte migration in vitro^[1][2].

The potency of UK-370106 (compound 7) for the inhibition of MMP-13 is 2.3 μM, some 100-fold less potent than its inhibition of MMP-3. UK-370106 is found to be inactive (IC₅₀>100 μM) vs zinc metalloproteases PCP and TACE and possesses the following inhibitory potencies vs MMP-2 (IC₅₀of 34.2 μM), MMP-7 (IC₅₀of 5.8 μM), MMP-8 (IC₅₀of 1.75 μM), MMP-9 (IC₅₀of 30.4 μM) and MMP-14 (IC₅₀of 66.9 μM)^[1].
UK-370106 potently inhibits cleavage of [³H]-fibronectin by MMP-3 (IC₅₀of 320 nM) but does not inhibit cleavage of [³H]-gelatin by either MMP-2 or -9 up to the highest concentration tested (100 μM)^[1].
UK-370106 is not cytotoxic to, nor affected proliferation of, fibroblasts, keratinocytes, or endothelial cells at 50-100 μM in vitro^[1].

Following iv (rat; 2 mg/kg) or topical administration to dermal wounds (rabbit), UK-370106 (compound 7) is cleared rapidly (t_1/2= 23 min) from plasma, but slowly (t_1/2approximately 3 days) from dermal tissue. In a model of chronic dermal ulcers, topical administration of UK-370106 for 6 days substantially inhibits MMP-3 ex vivo^[1].

572.73

Solid

C₃₅H₄₄N₂O₅

230961-21-4

Room temperature in continental US; may vary elsewhere.

DMSO : 200 mg/mL(349.20 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℃, 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: ≥ 5 mg/mL (8.73 mM); Clear solution

  此方案可获得 ≥ 5 mg/mL (8.73 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 50.0 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-CDin saline)

  Solubility: ≥ 5 mg/mL (8.73 mM); Clear solution

  此方案可获得 ≥ 5 mg/mL (8.73 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 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: ≥ 5 mg/mL (8.73 mM); Clear solution

  此方案可获得 ≥ 5 mg/mL (8.73 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。