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| ln Vivo |
Treatment with hPTH(1-38) at 200 μg/kg/day for 15 days (short-term) significantly increased trabecular bone area, thickness, and number in both primary and secondary spongiosa of the proximal tibial metaphysis compared to immobilization (IM) controls, despite continuous immobilization. [1]
Longer treatment (75 days) further increased trabecular bone area (+115% vs age-related controls, +435% vs IM controls), thickness (+58% vs age-related, +114% vs IM), and number (+38% vs age-related, +148% vs IM) in primary spongiosa. In secondary spongiosa, 75-day treatment increased bone area (+246% vs age-related, +419% vs IM), thickness (+190% vs age-related, +240% vs IM), and number (+24% vs age-related, +58% vs IM). [1] Short-term PTH treatment significantly increased labeling perimeter (+95% vs IM, +91% vs age-related), mineral apposition rate (+59% vs IM, +84% vs age-related), and tissue referent bone formation rate (+271% vs IM, +457% vs age-related) in secondary spongiosa. It also stimulated longitudinal bone growth (7.4 ± 0.3 μm/day vs IM controls 4.6 ± 0.2 μm/day at day 45). [1] Longer treatment (75 days) showed lower bone formation indices than short-term group but still higher than controls: labeling perimeter (+81% vs IM, +77% vs age-related), mineral apposition rate (+17% vs IM, +13% vs age-related), tissue referent bone formation rate (+152% vs IM, +211% vs age-related). Eroded perimeter was not altered by PTH treatment compared to IM controls. [1] |
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| Animal Protocol |
Female Sprague-Dawley rats (6-month-old, ~257 g) were acclimated for 7 days, then right hindlimbs were immobilized by bandaging to the abdomen for 30 days to induce osteopenia. After 30 days of immobilization, rats were subcutaneously injected daily with hPTH(1-38) at 200 μg/kg/day for 15 days (sacrificed at experimental day 45) or 75 days (sacrificed at day 105). The vehicle consisted of citric acid (192.1 mg), Na2HPO4 (331.2 mg), and NaCl (764.0 mg) in 100 ml distilled water. Injection volume was 0.5 ml/kg, adjusted weekly based on body weight. All rats received triple fluorochrome labeling: xylenol orange (90 mg/kg) on day 30 (before PTH treatment), achromycin tetracycline hydrochloride (25 mg/kg) at 14 and 13 days before sacrifice, and calcein (10 mg/kg) at 4 and 3 days before sacrifice. Rats were sacrificed under ketamine hydrochloride and xylazine anesthesia via cardiac puncture. Right tibiae were removed, fixed in 10% phosphate-buffered formalin, stained in Villanueva osteochrome stain for 5 days, dehydrated, embedded in methylmethacrylate, cut into 220 μm frontal sections, and ground to 20 μm for static and dynamic histomorphometric measurements. Primary spongiosa (within 1 mm from growth plate-metaphyseal junction) and secondary spongiosa (1-4 mm distal) were analyzed using a Digitizing Image Analysis System. [1]
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| Toxicity/Toxicokinetics |
No significant toxicity data reported. Body weight of hPTH(1-38)-treated rats did not differ from IM controls at day 45, but was significantly higher than IM controls and not different from age-related controls at day 105 (279 ± 6.9 g vs IM 270 ± 6.7 g). Gastrocnemius and soleus muscle weights in PTH-treated immobilized limbs did not significantly differ from those of vehicle-treated IM controls. [1]
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| References | |
| Additional Infomation |
hPTH(1-38) is a powerful anabolic bone agent that can overcome disuse-induced bone loss. It restored and added extra cancellous bone to the established disuse-osteopenic proximal tibial metaphysis in continuously immobilized rat hindlimbs. The mechanism involves enhanced osteoblast recruitment and activity (increased labeled perimeter, mineral apposition rate, bone formation rate) without altering eroded perimeter (bone resorption index). PTH also stimulated longitudinal bone growth, possibly contributing to greater cancellous bone mass in primary spongiosa. The study suggests that PTH may be useful for treating disuse-induced osteoporosis in humans. [1]
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| Molecular Formula |
C197H319N59O55S2
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|---|---|
| Molecular Weight |
4458.14
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| Exact Mass |
4457.349
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| CAS # |
78232-94-7
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| PubChem CID |
155923209
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
64
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| Hydrogen Bond Acceptor Count |
66
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| Rotatable Bond Count |
157
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| Heavy Atom Count |
313
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| Complexity |
10700
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| Defined Atom Stereocenter Count |
37
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC2=CNC=N2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC3=CNC4=CC=CC=C43)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC5=CNC=N5)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC6=CC=CC=C6)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)N
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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 |
| 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 | 0.2243 mL | 1.1215 mL | 2.2431 mL | |
| 5 mM | 0.0449 mL | 0.2243 mL | 0.4486 mL | |
| 10 mM | 0.0224 mL | 0.1122 mL | 0.2243 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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