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pTH (1-34) (rat)|PARATHYROID HORMONE (1-34),RAT is a peptide-based agonist of parathyroid hormone (PTH) receptor. It is able to increase serum PTH levels and bone mass in rats. Also can improve cortical and cancellous bone structure.
| Targets |
PTH1R (in vitro rat adenoid membrane adenylate cyclase stimulation assay: 24,800 IU/mg) [1]
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|---|---|
| ln Vitro |
In vitro adenylate cyclase stimulation assay using rat adenoid membrane showed that Parathyroid Hormone (1-34), Rat has a specific activity of 24,800 IU/mg. [1]
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| ln Vivo |
Bone formation is promoted by parathyroid hormone (1-34) (rat) administered subcutaneously at a dose of 40 mg/kg every day for four weeks [1].
In ovariectomized (Ovx) rats, subcutaneous administration of Parathyroid Hormone (1-34), Rat at 40 μg/kg per day for 4 weeks preserved cancellous bone volume (Cn-BV/TV) and trabecular connectivity when given preventively (starting 1 week post-Ovx). In curative mode (starting 3 or 5 weeks post-Ovx), Parathyroid Hormone (1-34), Rat alone prevented further loss of connectivity and Cn-BV/TV. Combined with 17β-estradiol (30 μg/kg per day), the treatment resulted in up to 300% improvement in node-to-node strut length (a connectivity parameter) and a 106% increase in Cn-BV/TV relative to bone status at treatment initiation. Parathyroid Hormone (1-34), Rat increased serum 1,25(OH)₂D concentration by 87-113% in Ovx rats across all treatment periods. It also elevated serum osteocalcin levels by 24-58% compared to Ovx+Vehicle groups. Bone formation rate was increased by 40-65% with PTH alone compared to Ovx+Vehicle. Trabecular thickness was increased by 25-40% with PTH treatment. Bone mineral density (BMD) at the distal femur (cancellous bone-enriched region) improved by 9-15% with PTH alone compared to untreated Ovx groups, while diaphyseal BMD showed little change. [1] |
| Animal Protocol |
Animal/Disease Models: Ovariectomized (Ovx) rat [1]
Doses: 40 mg/kg Route of Administration: SC, daily, for 4 weeks Experimental Results: Preserved Cn-BV/TV and trabecular connectivity, combined with estrogen and PTH 40% incremental Cn-BV/TV while maintaining trabecular connectivity comparable to that observed in orthopedically operated animals. Preventing further loss of connectivity and Cn-BV/TV, the combination of estrogen and PTH improved one of the trabecular connectivity parameters (node-to-node strut length) by 300% and increased Cn-BV/TV by 106%, regarding Bone status at the start of treatment. Female Sprague-Dawley rats (5 months old, ~275 g) were ovariectomized or sham-operated. Parathyroid Hormone (1-34), Rat was dissolved in 1 mM HCl and administered subcutaneously at 40 μg/kg per day. Treatments were initiated at 1, 3, or 5 weeks after surgery and lasted for 4 weeks. Rats were fed 15 g per day of rodent chow to prevent hyperphagia. Two doses of demecolcysteine (10 mg/kg) were given 6 and 2 days before killing. Before killing, 24-hour urine samples were collected using metabolic cages. Blood was collected via abdominal aorta 24 hours after the last injection. Right tibias and femurs were excised and fixed in 70% alcohol for histomorphometry and BMD measurements. [1] |
| References |
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| Additional Infomation |
Parathyroid Hormone (1-34), Rat administered intermittently acts as an anabolic agent for bone formation, increasing bone formation rate without further elevating osteoclast surface in Ovx rats. When combined with estrogen, the treatment achieves simultaneous high bone formation (via PTH) and inhibition of bone resorption (via estrogen), leading to superior restoration of cancellous bone volume and trabecular connectivity. This combination shows potential for curing established osteoporosis in an animal model. The effects were observed in both preventive (starting week 1) and curative (starting week 3 or 5) modes. No evidence of cortical bone loss was noted in this short-term rat study. [1]
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| Molecular Formula |
C180H291N55O48S2
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|---|---|
| Molecular Weight |
4057.70627617836
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| Exact Mass |
4056.149
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| CAS # |
98614-76-7
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| Related CAS # |
Parathyroid hormone (1-34) (rat) acetate
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| PubChem CID |
131954587
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| Appearance |
White to light yellow solid powder
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| LogP |
-16.8
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| Hydrogen Bond Donor Count |
58
|
| Hydrogen Bond Acceptor Count |
59
|
| Rotatable Bond Count |
143
|
| Heavy Atom Count |
285
|
| Complexity |
9570
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C)CCC(C(NC(C(NC(CC(N)=O)C(NC(C(NCC(NC(C(NC(CC1=CNC=N1)C(NC(C(NC(C)C(NC(CO)C(NC(C(NC(CCC(=O)O)C(NC(C(NC(CCSC)C(NC(CCC(N)=O)C(NC(CC1=CNC2C=CC=CC1=2)C(NC(C(NC(C(NC(C(NC(C(NC(C(NC(C(NC(CC(=O)O)C(NC(C(NC(C(NC(C(NC(C(=O)O)CC1C=CC=CC=1)=O)CC(N)=O)=O)CC1=CNC=N1)=O)C(C)C)=O)=O)CCC(N)=O)=O)CC(C)C)=O)CCCCN)=O)CCCCN)=O)CCCNC(=N)N)=O)CC(C)C)=O)=O)=O)=O)CCCNC(=N)N)=O)=O)C(C)C)=O)=O)=O)CC(C)C)=O)=O)CCCCN)=O)=O)CC(C)C)=O)=O)CC1=CNC=N1)=O)NC(C(CC(C)C)NC(C(CCC(N)=O)NC(C(C(C)CC)NC(C(CCC(=O)O)NC(C(CO)NC(C(C(C)C)NC(C(C)N)=O)=O)=O)=O)=O)=O)=O
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| InChi Key |
QSJWQIQDNBBZSH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C180H291N55O48S2/c1-23-96(18)145(235-160(264)115(50-55-140(246)247)212-172(276)131(83-236)231-176(280)142(93(12)13)232-146(250)97(19)184)177(281)216-113(48-53-135(187)240)157(261)219-121(68-91(8)9)164(268)214-117(57-64-285-22)159(263)224-125(73-102-80-195-86-202-102)167(271)225-127(75-136(188)241)169(273)217-118(65-88(2)3)148(252)200-82-138(243)205-106(41-29-32-58-181)149(253)223-124(72-101-79-194-85-201-101)166(270)220-119(66-89(4)5)161(265)204-98(20)147(251)230-132(84-237)173(277)234-143(94(14)15)174(278)215-114(49-54-139(244)245)154(258)208-109(44-35-61-197-179(190)191)152(256)213-116(56-63-284-21)158(262)210-111(46-51-133(185)238)155(259)222-123(71-100-78-199-105-40-28-27-39-104(100)105)165(269)221-122(69-92(10)11)162(266)209-110(45-36-62-198-180(192)193)151(255)206-107(42-30-33-59-182)150(254)207-108(43-31-34-60-183)153(257)218-120(67-90(6)7)163(267)211-112(47-52-134(186)239)156(260)227-129(77-141(248)249)171(275)233-144(95(16)17)175(279)228-126(74-103-81-196-87-203-103)168(272)226-128(76-137(189)242)170(274)229-130(178(282)283)70-99-37-25-24-26-38-99/h24-28,37-40,78-81,85-98,106-132,142-145,199,236-237H,23,29-36,41-77,82-84,181-184H2,1-22H3,(H2,185,238)(H2,186,239)(H2,187,240)(H2,188,241)(H2,189,242)(H,194,201)(H,195,202)(H,196,203)(H,200,252)(H,204,265)(H,205,243)(H,206,255)(H,207,254)(H,208,258)(H,209,266)(H,210,262)(H,211,267)(H,212,276)(H,213,256)(H,214,268)(H,215,278)(H,216,281)(H,217,273)(H,218,257)(H,219,261)(H,220,270)(H,221,269)(H,222,259)(H,223,253)(H,224,263)(H,225,271)(H,226,272)(H,227,260)(H,228,279)(H,229,274)(H,230,251)(H,231,280)(H,232,250)(H,233,275)(H,234,277)(H,235,264)(H,244,245)(H,246,247)(H,248,249)(H,282,283)(H4,190,191,197)(H4,192,193,198)
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| Chemical Name |
5-[[1-[[5-amino-1-[[1-[[1-[[1-[[4-amino-1-[[1-[[2-[[6-amino-1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[5-amino-1-[[1-[[1-[[1-[[6-amino-1-[[6-amino-1-[[1-[[5-amino-1-[[1-[[1-[[1-[[4-amino-1-[(1-carboxy-2-phenylethyl)amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-[[2-[[2-(2-aminopropanoylamino)-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2464 mL | 1.2322 mL | 2.4644 mL | |
| 5 mM | 0.0493 mL | 0.2464 mL | 0.4929 mL | |
| 10 mM | 0.0246 mL | 0.1232 mL | 0.2464 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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