货号	规格	价格	上海	北京	珠海	重庆	武汉
S88593-5mg买3赠1	99.80%	￥476.00 S88593-5mg ￥476.00 现货（买3赠1）	6 6	-	-	-	-
S88593-10mg买3赠1	99.80%	￥748.00 S88593-10mg ￥748.00 现货（买3赠1）	6 6	-	-	-	-
S88593-25mg促销	99.80%	￥1420.00 ￥1130.00 S88593-25mg ￥1130.00 现货	5 5	-	-	-	-
S88593-50mg促销	99.80%	￥2210.00 ￥1760.00 S88593-50mg ￥1760.00 现货	4 4	-	-	-	-
S88593-100mg促销	≥98%	￥3220.00 ￥2570.00 S88593-100mg ￥2570.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

LIT-927 is an orally active CXCL12 neutraligand (Ki: 267 nM for CXCL12 binding to CXCR4).

靶点：

CXCR

体外研究：

LIT-927 at 10 μM is able to inhibit the increase in intracellular calcium concentration in EGFP-CXCR4+ HEK cells in response to CXCL12, while it has no effect on calcium responses triggered by either CCL17 or CCL22 on EGFP-CCR4+ HEK cells, CCL5 on EGFP-CCR5+ HEK cells, or CCL2 on EGFPCCR2+ HEK cells

体内研究：

LIT-927 (350 μmol/kg) inhibited eosinophil infiltration by 54% and 55%. LIT-927 did not exhibit any side effects. In the same murine model of hypereosinophilia, LIT-927 (1400 μmol/kg, P.O.) shows a large and statistically reliable inhibition of eosinophil recruitment (62% inhibition)

细胞实验：

HEK EGFP-CXCR4-expressing cells were washed with phosphate-buffered saline (PBS) and detached in PBS-EDTA (5 mM) for 2 min at room temperature. Then cells were carefully resuspended in complete growth medium, pelleted by centrifugation at 320 × g for 5 min, and resuspended in HEPES buffer (137.5 mM NaCl, 6 mM KCl, 1.25 mM CaCl2, 1.25 mM MgCl2, 0.4 mM NaH2PO4, 5.6 mM glucose, 10 mM HEPES (pH 7.4) containing 0.1% BSA. Cells were used at a concentration of 10^6 cells/mL, then the cell suspension (1 mL) was transferred into a quartz cuvette. Time-based recordings of the fluorescence emitted at 510 nm (excitation at 470 nm) were performed at 21 °C using a Fluorolog 3 spectrofluorometer. Fluorescence binding measurements were initiated by adding at t = 150 s, 100 nM CXCL12-Texas Red (TR) to the 1 mL cell suspension. Binding of CXCL12-TR to EGFP-labeled CXCR4 was detected as a reversible decline of emission at 510 nm due to energy transfer from excited EGFP to TR. In the 'neutraligand protocol', CXCL12-TR was preinc

动物实验：

The activity of each compound was assessed in vivo in an 8 day model of allergic eosinophilic airway inflammation as described previously. Briefly, 9 week-old male Balb/c mice were sensitized by intraperitoneal injection of 50 μg of ovalbumin adsorbed on 2 mg of aluminum hydroxide in 0.1 mL of saline on days 0, 1, and 2. Mice were challenged intranasally [10 μg of OVA in 25 μL of saline (12.5 μL/nostril)] on days 5, 6, and 7. Control mice received intranasal administration of saline alone. Intranasal administrations were performed under anesthesia with intraperitoneal injection of ketamine (50 mg/kg) and xylazine (3.33 mg/kg). Food and water were supplied ad libitum. Two hours before each OVA or saline challenge, compounds in PBS/Cdx were administered intranasally (12.5 μL/nostril), intraperitoneally, or per os as indicated in the figure legends. Bronchoalveolar lavage (BAL) was performed 24 h after the last OVA or saline challenge as described. Mice were deeply anesthetized by intraperitoneal injection of ke

参考文献：

1. Regenass P, et al. Discovery of a Locally and Orally Active CXCL12 Neutraligand (LIT-927) with Anti-inflammatory Effect in a Murine Model of Allergic Airway Hypereosinophilia. J Med Chem. 2018 Sep 13;61(17):7671-7686.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.042 ml	15.209 ml	30.418 ml
5 mM	0.608 ml	3.042 ml	6.084 ml
10 mM	0.304 ml	1.521 ml	3.042 ml
50 mM	0.061 ml	0.304 ml	0.608 ml

注意：

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参考文献

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