J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST₄ receptor) agonist with IC₅₀s of 0.05 nM and 0.07 nM for human and rat SST₄ receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats^[1][2].

IC50: 0.05 nM (human SST₄) and 0.07 nM (rat SST₄)^[1]

J-2156 TFA binds with nanomolar affinity to the human somatostatin receptor subtype 4 (hsst₄: K_i=1.2 nM) and is over 400-fold subtype-selective against the other somatostatin receptors (hsst₁: K_i=0.5 μM; hsst₂: K_i>5 μM; hsst₃: K_i=1.4 μM; hsst₅: K_i=0.54 μM) in Chinese hamster ovary (CHO) cells^[2].

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

J-2156 TFA (1-10 mg/kg; i.p.; for 3 hours) of single bolus doses has anti-allodynic effect on ipsilateral and contralateral in BCIBP-rats^[1].

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

582.59

C₂₆H₂₉F₃N₄O₆S

2387505-73-7

Room temperature in continental US; may vary elsewhere.

Protect from light, stored under nitrogen

Powder	-80deg;C	2 years
	-20deg;C	1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from light, stored under nitrogen)

In Vitro:;

H₂O : 100 mg/mL (171.65 mM; Need ultrasonic)

DMSO : 100 mg/mL (171.65 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 (protect from light, stored under nitrogen)。-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。

In Vivo:

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 (4.29 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.29 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 (4.29 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.29 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 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 (4.29 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.29 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]. Shenoy PA, et al. The Somatostatin Receptor-4 Agonist J-2156 Alleviates Mechanical Hypersensitivity in a Rat Model of Breast Cancer Induced Bone Pain. Front Pharmacol. 2018 May 15;9:495.

  [2]. Mia Engström, et al. Superagonism at the Human Somatostatin Receptor Subtype 4. J Pharmacol Exp Ther. 2005 Jan;312(1):332-8.