Lubabegron
(Synonyms: LY-488756) 目录号 : GC67977Lubabegron 是一种有效的 β-肾上腺素受体 (β-AR) 调节剂。Lubabegron 在牛中表现出对 β1 和 β2 受体亚型的拮抗行为和对 β3 受体亚型的激动行为。Lubabegron 可减少动物或其废物的 NH3 气体排放。
Cas No.:391920-32-4
Sample solution is provided at 25 µL, 10mM.
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Lubabegron is a potent modulator of β-adrenergic receptor (β -AR). Lubabegron demonstrates antagonistic behavior at the β1 and β 2 receptor subtypes and agonistic behavior at the β 3 receptor subtype in cattle. Lubabegron reduces NH3 gas emissions from an animal or its waste[1].
[1]. Kube JC, et al. Effects of various doses of lubabegron on calculated ammonia gas emissions, growth performance, and carcass characteristics of beef cattle during the last 56 days of the feeding period [published correction appears in Transl Anim Sci. 2021 Nov 15;5(4):txab210]. Transl Anim Sci. 2021;5(3):txab137.
| Cas No. | 391920-32-4 | SDF | Download SDF |
| 别名 | LY-488756 | ||
| 分子式 | C29H29N3O3S | 分子量 | 499.62 |
| 溶解度 | DMSO : 100 mg/mL (200.15 mM; Need ultrasonic) | 储存条件 | 4°C, away from moisture and light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0015 mL | 10.0076 mL | 20.0152 mL |
| 5 mM | 0.4003 mL | 2.0015 mL | 4.003 mL |
| 10 mM | 0.2002 mL | 1.0008 mL | 2.0015 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Lubabegron fumarate acts as a β-adrenergic receptor antagonist in cultured bovine intramuscular and subcutaneous adipocytes
J Anim Sci 2022 Mar 1;100(3):skac052.PMID:35262701DOI:10.1093/jas/skac052.
We hypothesized that Lubabegron fumarate (LUB) (Experior, Elanco Animal Health, Greenfield, IN) would act as an antagonist to β-adrenergic receptor (β-AR) subtypes in primary bovine subcutaneous (s.c.) and intramuscular (i.m.) adipocytes differentiated in culture. This study employed LUB, dobutamine (DOB, a selective β1-agonist), salbutamol (SAL, a selective β2-agonist), and propranolol (PRO, a non-selective β-AR antagonist). Preadipocytes were isolated by standard techniques from bovine longissimus muscle and overlying s.c. adipose tissue and differentiated to adipocytes for 14 d. The adipocyte source x stage of differentiation interaction was significant for β-adrenergic receptors-1 (ADRB1) (P = 0.001) and ADRB2 (P = 0.01) in that expression of ADRB1 and ADRB2 was greater in s.c. adipocytes than in s.c. preadipocytes; expression of the ADRB1-3 did not change after differentiation of i.m. adipocytes. CCATT/enhancer-binding protein alpha (CEBPA) expression increased upon differentiation in both s.c. and i.m. adipocytes (P = 0.006). The source x stage of differentiation interaction was significant for peroxisome proliferator-activated receptor gamma (PPARG) (P ≤ 0.001) and fatty acid binding protein-4 (FABP4) (P = 0.004). Expression of PPARG increased after differentiation of s.c. preadipocytes to adipocytes, but PPARG expression did not change with differentiation of i.m. preadipocytes to adipocytes. FABP4 expression increased after differentiation of both s.c. and i.m. adipocytes, but FABP4 expression increased to a greater extent in s.c. adipocytes. In s.c. adipocytes, DOB elevated cAMP and glycerol production and protein kinase A (PKA) activity, and SAL increased PKA activity; these effects were abolished by LUB and PRO (P < 0.001). Incubation of i.m. adipocytes with SAL increased cAMP production and PKA activity, which was attenuated by LUB and PRO (P ≤ 0.006). In s.c. adipocytes, SAL, LUB + SAL, and LUB + DOB upregulated hormone sensitive lipase (HSL) (P < 0.001) and perilipin (P = 0.002) gene expression. In i.m. adipocytes, DOB and LUB + DOB increased HSL gene expression (P = 0.001) and LUB + SAL depressed adipose triglyceride lipase expression below control levels (P = 0.001). These results demonstrate that LUB is a β-AR antagonist at the β1-AR and β2-AR subtypes in s.c. adipocytes, and that s.c. and i.m. exhibit different responses to β-AA and LUB.
Effects of feeding Lubabegron on gas emissions, growth performance, and carcass characteristics of beef cattle housed in small-pen environmentally monitored enclosures during the last 3 mo of the finishing period
J Anim Sci 2021 Dec 1;99(12):skab338.PMID:34849995DOI:10.1093/jas/skab338.
The development of technologies that promote environmental stewardship while maintaining or improving the efficiency of food animal production is essential to the sustainability of producing a food supply to meet the demands of a growing population. As such, Elanco (Greenfield, IN) pursued an environmental indication for a selective β-modulator (Lubabegron; LUB). LUB was recently approved by the United States Food and Drug Administration (FDA) to be fed to feedlot cattle during the last 14 to 91 d of the feeding period for reductions in gas emissions/kg of unshrunk final BW and HCW. A 4 × 2 factorial arrangement of treatments was used with the factors of dose (0.0, 1.38, 5.5, or 22.0 mg·kg-1 DM basis) and sex (steers or heifers). Three 91-d cycles were conducted (112 cattle/cycle) with each dose × sex combination being represented by a single cattle pen enclosure (CPE; 14 cattle/CPE) resulting in a total of 168 steers and 168 heifers (n = 6 replicates/dose). There were no interactions observed between dose and sex for any variable measured in the study (P ≥ 0.063). Five gases were evaluated for all pens based on CPE concentrations relative to ambient air: NH3, CH4, N2O, H2S, and CO2. Cumulative NH3 gas emissions were reduced by feeding cattle 5.5 and 22.0 mg·kg-1 LUB (P ≤ 0.023) and tended (P = 0.076) to be lower for the cattle fed 1.38 mg·kg-1 LUB compared with the negative controls (CON). The cumulative NH3 gas emission reductions of 960 to 1032 g, coupled with HCW increases (P ≤ 0.019) of 15 to 16 kg for all LUB doses vs. CON, led to reductions in NH3 gas emissions/kg HCW for all three LUB treatments (P ≤ 0.004). Similar to HCW, reductions in NH3 gas emissions/kg of unshrunk final BW were observed for all LUB doses (P ≤ 0.009) and were attributable to both decreases in NH3 gas emissions and numerical increases in BW. Dose had no effect on cumulative emissions or emissions standardized by BW or HCW for the other four gases (P ≥ 0.268). LUB is a novel tool to reduce emissions of NH3 gas per kilogram of unshrunk live BW and hot carcass weight.
Effects of various doses of Lubabegron on calculated ammonia gas emissions, growth performance, and carcass characteristics of beef cattle during the last 56 days of the feeding period
Transl Anim Sci 2021 Aug 21;5(3):txab137.PMID:34532643DOI:10.1093/tas/txab137.
Lubabegron (LUB; Experior, Elanco, Greenfield, IN, USA) was approved by the U.S. Food and Drug Administration in 2018 and is indicated for the reduction of ammonia (NH3) gas emissions·kg-1 body weight (BW) and hot carcass weight (HCW) when fed to feedlot cattle during the final 14 to 91 d of the finishing period. LUB demonstrates antagonistic behavior at the β 1 and β 2 receptor subtypes and agonistic behavior at the β 3 receptor subtype in cattle and is classified by the Center for Veterinary Medicine as a "beta-adrenergic agonist/antagonist." This report describes a randomized complete block study that evaluated LUB dose (0, 1.5, 3.5, and 5.5 mg·kg-1 dry matter) during the last 56 d of the feeding period on calculated NH3 gas emissions, live weight, carcass weight, and associated ratios in beef feedlot cattle. Carcass characteristics, mobility, and health were also evaluated. All cattle received monensin and tylosin throughout the study. Ammonia gas emissions were calculated using the equation developed by Brown et al. (Brown, M. S., N. A. Cole, S. Gruber, J. Kube, and J. S. Teeter. 2019. Modeling and prediction accuracy of ammonia gas emissions from feedlot cattle. App. Anim. Sci. 35:347-356). The reduction in calculated cumulative NH3 gas emissions with LUB ranged from 1.3% to 11.0% (85 to 708 g/hd). When NH3 gas emissions were expressed on a live weight (unshrunk) and carcass weight basis, calculated NH3 gas emissions decreased by 3.0% to 12.8% and 3.8% to 14.6%, respectively. Daily dry matter intake was 2.3% greater (P trt < 0.05) for steers that received LUB. Average daily gain was 13.7% greater (P trt < 0.05; 1.68 vs. 1.91 kg), while gain efficiency was 10.8% greater (P trt < 0.05; 0.167 vs. 0.185) for steers fed LUB. Animal mobility was scored in the pen approximately 1 wk prior to harvest, when cattle were loaded on trucks scheduled for harvest, and at antemortem inspection during lairage. No treatment differences (P trt ≥ 0.170) were observed at any time for the percent of cattle receiving mobility scores of 1 or 2 (normal or minor stiffness but moving with the normal cattle, respectively). Cattle mobility scored as a 1 or 2 equaled or exceeded 92% at all times. Final BW and HCW increased (P trt < 0.05) 11.6 to 15.7 kg and 11.3 to 17.1 kg, respectively, in cattle receiving LUB compared to cattle receiving monensin plus tylosin alone.
Erratum to: Effects of various doses of Lubabegron on calculated ammonia gas emissions, growth performance, and carcass characteristics of beef cattle during the last 56 days of the feeding period
Transl Anim Sci 2021 Nov 15;5(4):txab210.PMID:34805772DOI:10.1093/tas/txab210.
[This corrects the article DOI: 10.1093/tas/txab137.].
Characterization of β-adrenergic receptors in bovine intramuscular and subcutaneous adipose tissue: comparison of Lubabegron fumarate with β-adrenergic receptor agonists and antagonists
J Anim Sci 2021 Aug 1;99(8):skab116.PMID:34337647DOI:10.1093/jas/skab116.
Chinese hamster ovary cell constructs expressing either the β 1-, β 2- or β 3-adrenergic receptor (AR) were used to determine whether a novel β-AR modulator, Lubabegron fumarate (LUB; Experior, Elanco Animal Health) might exert greater potency for a specific β-AR subtype. EC50 values calculated based on cAMP accumulation in dose response curves indicate that LUB is highly selective for the β 3-AR subtype, with an EC50 of 6 × 10-9 M, with no detectible agonistic activity at the β 2-AR. We hypothesized that the accumulation of lipolytic markers would reflect the agonist activity at each of the β-receptor subtypes of the specific ligand; additionally, there would be differences in receptor subtype expression in subcutaneous (s.c.) and intrmuscular (i.m.) adipose tissues. Total RNA was extracted from adipose tissue samples and relative mRNA levels for β 1-, β2-, and β 3-AR were measured using real-time quantitative polymerase chain reaction. Fresh s.c. and i.m. adipose tissue explants were incubated with isoproterenol hydrochloride (ISO; β-AR pan-agonist), dobutamine hydrochloride (DOB; specific β 1-AA), salbutamol sulfate (SAL; specific β 2-AA), ractopamine hydrochloride (RAC), zilpaterol hydrochloride (ZIL), BRL-37344 (specific β 3-agonist), or LUB for 30 min following preincubation with theophylline (inhibitor of phosphodiesterase). Relative mRNA amounts for β 1-, β 2-, and β 3-AR were greater (P < 0.05) in s.c. than in i.m. adipose tissue. The most abundant β-AR mRNA in both adipose tissues was the β 2-AR (P < 0.05), with the β 1- and β 3-AR subtypes being minimally expressed in i.m. adipose tissue. ISO, RH, and ZH stimulated the release of glycerol and nonesterified fatty acid (NEFA) from s.c. adipose tissue, but these β-AR ligands did not alter concentrations of these lipolytic markers in i.m. adipose tissue. LUB did not affect glycerol or NEFA concentrations in s.c. or i.m. adipose tissue, but attenuated (P < 0.05) the accumulation of cAMP mediated by the β 1- and β 2-AR ligands DOB and SAL in s.c. adipose tissue. Collectively, these data indicate that bovine i.m. adipose tissue is less responsive than s.c. adipose tissue to β-adrenergic ligands, especially those that are agonists at the β 1- and β3-receptor subtypes. The minimal mRNA expression of the β 1- and β 3 subtypes in i.m. adipose tissue likely limits the response potential to agonists for these β-AR subtypes.